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Melatonin MT Receptor agonist

Name: Melatonin
Brand: Selleck Chemicals
SKU: S1204
Rating: 5 (34 reviews)

Cat.Nr.S1204

Melatonin is een MT receptor-agonist, gebruikt als voedingssupplement. Deze verbinding is een selectieve ATF-6-remmer en downreguleert COX-2. Het versterkt mitophagy en reguleert de homeostase van apoptosis en autophagy.

Melatonin MT Receptor agonist Chemical Structure

Chemische structuur

Moleculair gewicht: 232.28

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Kwaliteitscontrole

Batch: Zuiverheid: 99.97%

99.97

Gerelateerde doelwitten	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Overige MT Receptor Inhibitoren	Luzindole

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
CHO	Function assay			Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1A expressed in CHO cells, Ki=0.00008μM	9435890
CHO	Function assay			Inhibition of the 2-[125I]- iodomelatonin binding to Melatonin receptor type 1B expressed in CHO cells, Ki=0.00012μM	9435890
NIH3T3	Function assay			Binding affinity was measured against cloned human Melatonin receptor type 1A subtype stably expressed in rat fibroblasts NIH3T3 cells, Ki=0.0002951μM	9733487
NIH 3T3	Function assay			Binding affinity towards recombinant human melatonin receptor type 1B expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00033μM	10737738
NIH 3T3	Function assay			Binding affinity towards recombinant human melatonin receptor type 1A expressed in NIH 3T3 cells using 2-[121I]iodomelatonin radioligand binding assay, Ki=0.00066μM	10737738
HEK293	Function assay			Binding affinity for human melatonin receptor type 1A, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.0002μM	11063602
HEK293	Function assay			Binding affinity for melatonin receptor type 1B, expressed in HEK293 cells (2-[125I]iodomelatonin is used as radioligand), Ki=0.00053μM	11063602
NIH 3T3	Function assay			Binding affinity towards melatonin receptor type 1B stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin, Ki=0.0002818μM	11520198
NIH 3T3	Function assay			Binding affinity towards melatonin receptor type 1A stably expressed in NIH3T3 rat fibroblast cells using 2-[125I]iodomelatonin (100 pM) as radioligand, Ki=0.0002884μM	11520198
HEK293	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1A expressed in HEK293 cells, Ki=0.00012μM	11960497
HEK293	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in HEK293 cells, Ki=0.00031μM	11960497
HEK293	Function assay			Binding affinity on human melatonin receptor type 1B stably transfected in human embryonic kidney (HEK 293) cells using 2-[125I]iodomelatonin as radioligand., Ki=0.00031μM	12061881
CHO	Function assay			Intrinsic activity at human Melatonin receptor type 1B evaluated on [35S]GTP-gamma-S, binding in Chinese hamster ovarian (CHO) cells, EC50=0.00047μM	12061881
CHO	Function assay			Intrinsic activity evaluated on [35S]GTP -gamma-S binding in hamster ovarian (CHO) cells, stably expressing human Melatonin receptor type 1A, EC50=0.00192μM	12061881
CHO	Function assay			Ability to inhibit 2-[125I]iodomelatonin specific binding to human melatonin receptor type 1A (MT1) expressed in CHO cells., Ki=0.0000823μM	12213062
CHO	Function assay			Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells, Ki=0.0000823μM	12213063
HEK293	Function assay			Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00014μM	12646022
HEK293	Function assay			Binding affinity for human Melatonin receptor type 1B stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=0.00041μM	12646022
NIH3T3	Function assay			Binding affinity against human MT2 melatonin receptor expressed in NIH3T3 cells, Ki=0.0003μM	14643330
NIH3T3	Function assay			Binding affinity against human MT1 melatonin receptor expressed in NIH3T3 cells., Ki=0.0004μM	14643330
NIH3T3	Function assay			Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0003μM	14980664
NIH3T3	Function assay			Binding of 2-[125I]iodomelatonin to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0004μM	14980664
NIH3T3	Function assay			Binding affinity for human recombinant Melatonin receptor type 2 expressed in NIH3T3 cells, Ki=0.0002818μM	15293992
NIH3T3	Function assay			Binding affinity for human recombinant Melatonin receptor type 1 expressed in NIH3T3 cells, Ki=0.0002884μM	15293992
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1A, Ki=0.0003μM	15380218
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to membrane preparations of NIH3T3 cells stably expressing human Melatonin receptor type 1B, Ki=0.0007μM	15380218
NIH3T3	Function assay			Binding affinity against Melatonin receptor type 1A stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0003μM	15713384
NIH3T3	Function assay			Binding affinity against Melatonin receptor type 1B stably expressed in NIH3T3 cells using 2-[125I]iodomelatonin, Ki=0.0007μM	15713384
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1B (MT2) expressed in NIH3T3 rat fibroblast cells , Ki=0.0002818μM	15943478
NIH3T3	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human melatonin receptor type 1A (MT1) expressed in NIH3T3 rat fibroblast cells, Ki=0.0002884μM	15943478
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.00035μM	16759094
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.00039μM	16759094
NIH3T3	Function assay	1 nM		Activity at MT1 receptor expressed in NIH3T3 cells assessed as inhibition of forskolin-stimulated cAMP synthesis at 1 nM	16759094
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in NIH3T3 cells, Ki=0.000257μM	17149869
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in NIH3T3 cells, Ki=0.0003236μM	17149869
NIH 3T3	Function assay			Displacement of 2[125I]iodomelatonin from recombinant human MT2 receptor expressed in NIH 3T3 cells, Ki=0.0003548μM	17346859
NIH 3T3	Function assay			Displacement of 2[125I]iodomelatonin from recombinant human MT1 receptor expressed in NIH 3T3 cells, Ki=0.000389μM	17346859
NIH3T3	Function assay			Displacement of 2[125I]iodomelatonin from human recombinant MT1 receptor expressed in NIH3T3 cells, Ki=0.000263μM	17459711
NIH3T3	Function assay			Displacement of 2[125I]iodomelatonin from human recombinant MT2 receptor expressed in NIH3T3 cells, Ki=0.0003388μM	17459711
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0002μM	17481904
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0003μM	17481904
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells, Ki=0.0001413μM	18052314
NIH3T3	Function assay			Displacement of 2-[125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells, Ki=0.0002399μM	18052314
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, IC50=0.0002μM	18372181
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in HEK293 cells, IC50=0.00053μM	18372181
CHO	Function assay			Displacement of [125I]iodomelatonin from MT3/QR2 melatonin binding site expressed in CHO cells, IC50=0.06457μM	18400335
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human melatonin MT1 receptor expressed in CHO cells, Ki=0.000525μM	18657980
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human melatonin MT2 receptor expressed in CHO cells, Ki=0.000741μM	18657980
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM	18778943
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00041μM	18778943
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay, EC50=0.00049μM	18778943
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM	19193160
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM	19193160
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00049μM	19329323
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding, EC50=0.00224μM	19329323
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells by gamma counting, Ki=0.0004571μM	19473848
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells by gamma counting, Ki=0.000955μM	19473848
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human melatonin MT1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000296μM	20227878
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human melatonin MT2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki=0.000429μM	20227878
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00049μM	20444610
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0022μM	20444610
NIH3T3	Function assay		90 mins	Displacement of [125I]iodomelatonin from human cloned MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003311μM	20674373
NIH3T3	Function assay		90 mins	Displacement of [125I]iodomelatonin from human cloned MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0006166μM	20674373
CHO-Galpha16	Function assay		20 mins	Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.00056μM	21237644
CHO-Galpha16	Function assay			Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells, Ki=0.00058μM	21237644
CHO-Galpha16	Function assay			Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells, Ki=0.00099μM	21237644
CHO-Galpha16	Function assay		20 mins	Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=0.0011μM	21237644
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00022μM	21392858
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00035μM	21392858
HEK293	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00025μM	21420861
HEK293	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00034μM	21420861
CHO	Function assay			Agonist activity at human MT2 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.00042μM	21420861
CHO	Function assay			Agonist activity at human MT1 receptor expressed in CHO cells by [35S]GTPgamma binding assay, EC50=0.0015μM	21420861
CHO	Function assay		30 mins	Agonist activity at human MT1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0000257μM	21473625
CHO	Function assay			Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting, Ki=0.00021μM	21473625
CHO	Function assay			Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by microscintillation counting, Ki=0.00024μM	21473625
CHO	Function assay		30 mins	Agonist activity at human MT2 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by EnVision Multilabel Plate Readers, EC50=0.0008511μM	21473625
CHO	Function assay		30 mins	Agonist activity at human MT1 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.000026μM	21568291
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.00021μM	21568291
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.00024μM	21568291
CHO	Function assay		30 mins	Agonist activity at human MT2 receptor expressed in CHO cells assessed as decrease in forskolin-stimulated cAMP release after 30 mins by multilabel plate reader, EC50=0.00082μM	21568291
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00025μM	21764185
HEK293	Function assay			Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in human HEK293 cells by radioligand binding assay, Ki=0.00034μM	21764185
NIH3T3	Function assay		90 mins	Displacement of 2-[125I]iodomelatonin from human MT1 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.000263μM	22047556
NIH3T3	Function assay		90 mins	Displacement of 2-[125I]iodomelatonin from human MT2 receptor expressed in rat NIH3T3 cells after 90 mins, Ki=0.0003388μM	22047556
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human MT1 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000296μM	23228808
CHO	Function assay		60 mins	Displacement of [3H]melatonin from human MT2 receptor expressed in CHO cells after 60 mins by microbeta scintillation method, Ki=0.000429μM	23228808
HEK293	Function assay		2 hrs	Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0002μM	23265885
HEK293	Function assay		2 hrs	Displacement of [125I]2-iodomelatonin from human recombinant MT2 receptor expressed in HEK293 cells after 2 hrs by gamma counting, Ki=0.0005μM	23265885
CHOK1	Function assay		3 hrs	Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, Ki=0.00011μM	23403082
CHOK1	Function assay		3 hrs	Displacement of [125I]2-iodomelatonin from human recombinant melatonin receptor 1 expressed in CHOK1 cells after 3 hrs, IC50=0.00021μM	23403082
CHO	Function assay		1 hr	Intrinsic activity at human melatonin MT2 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0004μM	24417958
CHO	Function assay		1 hr	Intrinsic activity at human melatonin MT1 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr, EC50=0.0017μM	24417958
Primary neural stem cells	Neurogenic assay	10 uM	48 hrs	Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring TuJ1 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry	24738476
Primary neural stem cells	Neurogenic assay	10 uM	48 hrs	Neurogenic activity in Wistar rat Primary neural stem cells assessed as cell maturation by measuring MAP-2 at 10 uM after 48 hrs by DAPI staining-based immunohistochemistry	24738476
HEK293	Function assay			Displacement of [125L]iodomelatonin from human MT1 receptor expressed in HEK293 cells, Ki=0.00014μM	24930835
HEK293	Function assay			Displacement of [125L]iodomelatonin from human MT2 receptor expressed in HEK293 cells, Ki=0.00041μM	24930835
HEK293	Function assay		120 mins	Displacement of 2-[125I]iodomelatonin from human MT1 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00014μM	25232966
HEK293	Function assay		120 mins	Displacement of 2-[125I]iodomelatonin from human MT2 receptor stably transfected in HEK293 cells after 120 mins by scintillation counting, Ki=0.00041μM	25232966
SH-SY5Y	Neuroprotective assay	10 uM	24 hrs	Neuroprotective activity against H2O2-induced oxidative stress-associated death in human SH-SY5Y cells assessed as increase in cell viability at 10 uM incubated for 24 hrs prior to H2O2 challenge measured after 24 hrs by MTT assay	26363866
HEK293	Function assay		120 mins	Displacement of [125I]2-Iodomelatonin from human MT1 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00025μM	26785296
HEK293	Function assay		120 mins	Displacement of [125I]2-Iodomelatonin from human MT2 receptor expressed in HEK293 cells after 120 mins by radioligand competition assay, Ki=0.00034μM	26785296
CHO	Function assay			Displacement of [125I]2-iodomelatonin from human recombinant ML1A receptor expressed in CHO cells, IC50=0.00011μM	26988801
PC12	Neuroprotective assay	10 uM	2 hrs	Neuroprotective activity against H2O2-induced damage in rat PC12 cells assessed as cell viability at 10 uM preincubated for 2 hrs followed by H2O2 addition for 24 hrs by MTT assay	27460699
PC12	Neuroprotective assay	20 uM	24 hrs	Neuroprotective activity against amyloid beta (1 to 42 residues) induced cell death in rat PC12 cells assessed as increase in cell viability at 20 uM preincubated for 24 hrs followed by amyloid beta (1 to 42 residues) addition measured after 24 hrs by MTT	27484514
CHO	Function assay		60 mins	Displacement of [125I]2-iodomelatonin from human recombinant MT1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method, IC50=0.00011μM	27876250
PC12	Neuroprotective assay	25 uM	2 hrs	Neuroprotective activity against H2O2-induced oxidative damage in rat PC12 cells assessed as increase in cell viability at 25 uM preincubated for 2 hrs followed by H2O2 challenge measured after 24 hrs by MTT assay	28800459
MDA-MB-231	Antiproliferative assay		24 hrs	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.9μM	29144746
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
HEK293	Function assay			Agonist activity at MT1 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.001μM	31204226
HEK293	Function assay			Agonist activity at MT2 receptor (unknown origin) expressed in HEK293 cells by Fluo-8 dye-based calcium assay, EC50=0.025μM	31204226
COS7	Function assay		1.5 hrs	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00018μM	31727472
NIH3T3	Function assay		90 mins	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.0002042μM	31727472
NIH3T3	Function assay		90 mins	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes incubated for 90 mins by Cheng-Prusoff equation analysis, Ki=0.000302μM	31727472
NIH3T3	Function assay			Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00033μM	31727472
CHO	Function assay		1 hr	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00046μM	31727472
NIH3T3	Function assay			Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in NIH3T3 cells membranes by radioligand binding assay, Ki=0.00066μM	31727472
COS7	Function assay		1.5 hrs	Displacement of 2-[1251]-iodomelatonin from human MT1 receptor expressed in COS7 cells incubated for 1.5 hrs by gamma counting method, Ki=0.00088μM	31727472
CHO	Function assay		1 hr	Displacement of 2-[1251]-iodomelatonin from human MT2 receptor expressed in CHO cells incubated for 1 hr by gamma counting method, Ki=0.00095μM	31727472
CHO	Function assay			Binding affinity against human Melatonin receptor type 1A by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00013μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells, Ki=0.0002μM	ChEMBL
CHO	Function assay			Binding affinity against human Melatonin receptor type 1B by displacement of [125I]iodomelatonin stably expressed in CHO cells, Ki=0.00023μM	ChEMBL
CHO	Function assay			Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells, Ki=0.00029μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells, Ki=0.0004571μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT1 receptor expressed in CHO cells by Gamma counting, Ki=0.0004571μM	ChEMBL
CHO	Function assay		1 hr	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT1 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.0004571μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells, Ki=0.000955μM	ChEMBL
CHO	Function assay			Displacement of 2-[125I]-iodomelatonin from human MT2 receptor expressed in CHO cells by Gamma counting, Ki=0.000955μM	ChEMBL
CHO	Function assay		1 hr	Displacement of 2-[125I]-iodomelatonin from human melatonin receptor MT2 expressed in CHO cells after 1 hr by gamma counting analysis, Ki=0.000955μM	ChEMBL
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Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	232.28	Formule	C₁₃H₁₆N₂O₂	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	73-31-4	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC 56423, N-Acetyl-5-methoxytryptamine,NSC 113928,MT			Smiles	CC(=O)NCCC1=CNC2=C1C=C(C=C2)OC

Oplosbaarheid

In vitro
Batch:

DMSO : 46 mg/mL (198.03 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 46 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%absolute ethyl alcohol 1 95%Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.300mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 46 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	10.000mg/ml (43.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	melatonin receptor
In vitro	Melatonin interageert met het zeer toxische hydroxylradicaal met een snelheidsconstante die equivalent is aan die van andere zeer efficiënte hydroxylradicaalvangers. Het neutraliseert naar verluidt waterstofperoxide, singletzuurstof, peroxynitriet anion, stikstofmonoxide en hypochloorzuur. Deze verbinding wordt verondersteld het zeer toxische hydroxylradicaal, het peroxynitriet anion en mogelijk het peroxylradicaal op te vangen. Het vangt naar verluidt het superoxide-anionradicaal op en het dooft singletzuurstof. De stof stimuleert de mRNA-niveaus voor superoxide dismutase en de activiteiten van glutathionperoxidase, glutathionreductase en glucose-6-fosfaatdehydrogenase (die allemaal antioxidatieve enzymen zijn), waardoor de antioxidatieve capaciteit toeneemt. Het is aangetoond dat deze chemische stof in celvrije systemen direct H2O2, singletzuurstof (1O2) en stikstofmonoxide (NO) opvangt, met weinig of geen vermogen om het superoxide-anionradicaal (O2-) in vitro op te vangen. Het ontgift ook direct het peroxynitriet anion (ONOO-) en/of peroxynitrietzuur (ONOOH), of de geactiveerde vorm van dit molecuul, ONOOH*. Melatonin werkt als een directe vrije radicaalvanger met het vermogen om zowel reactieve zuurstof- als reactieve stikstofspecies te ontgiften. Het remt cAMP-accumulatie in de meeste onderzochte cellen, maar de indole-effecten op andere boodschappers zijn tot nu toe vaak alleen waargenomen in één type cellen of weefsel. Deze verbinding reguleert ook de transcriptiefactoren, namelijk fosforylering van cAMP-responsief elementbindend proteïne en expressie van c-Fos.
In vivo	Melatonin verbetert necrotiserende enterocolitis door Th17/Treg-onbalans te voorkomen via activering van de AMPK/SIRT1-route
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/11060493/ [2] https://pubmed.ncbi.nlm.nih.gov/9770244/ [3] https://pubmed.ncbi.nlm.nih.gov/11898866/ [4] https://pubmed.ncbi.nlm.nih.gov/9674691/ [5] https://pubmed.ncbi.nlm.nih.gov/36225557/ [6] https://pubmed.ncbi.nlm.nih.gov/32685016/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Western blot	MT1 / MT2 / p-CREB / CREB / BDNF p-Raf / p-ERK / p-p90RSK / PKAα / p-AKT / p-JNK / p-CaMKII		29570621

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT04521972	Not yet recruiting	Pregnancy Related\|Labor; Poor\|Uterine Contractions Weak	Michigan State University\|McLaren Health Care	October 1 2024	Not Applicable
NCT06390267	Not yet recruiting	Acute Stress Reaction\|Cognitive Performance	Spark Biomedical Inc.\|Battelle Memorial Institute	August 2024	Not Applicable
NCT06343805	Not yet recruiting	Primary Myelofibrosis\|Post-Essential Thrombocythemia Myelofibrosis\|Post-Polycythemia Vera Myelofibrosis\|PMF\|PPV-MF\|PET-MF	Ajax Therapeutics Inc.	July 15 2024	Phase 1

Technische ondersteuning

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