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Cat.nr.: S1985
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0301μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0631μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2, EC50=0.085μM. | 11985476 | |||
| 1321N1 | Function assay | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay, EC50=0.085μM. | 19419868 | |||
| 1321N1 | Function assay | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C, EC50=0.085μM. | 17302398 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0958μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.111μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.12μM. | 19419204 | |||
| MDCK | Function assay | 10 uM | Induction of intracellular calcium level in MDCK cells assessed as net peak value at 10 uM by Fura-2 in calcium free medium, Activity=0.132μM. | 23163425 | ||
| 1321N1 | Function assay | 30 mins | Agonist activity at GFP tagged-human P2Y1 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=0.15μM. | 21090681 | ||
| NG108-15 | Function assay | Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin), EC50=0.18μM. | 29254895 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.183μM. | 19419204 | |||
| HEK293 | Function assay | Agonist activity at P2Y1 receptor expressed in human HEK293 cells, EC50=0.2μM. | 20175517 | |||
| HEK293 | Function assay | Agonist activity at rat P2Y1R expressed in HEK293 cells assessed as release of intracellular calcium by fluorescence based assay, EC50=0.2μM. | 22873688 | |||
| CF/T43 | Function assay | Agonist activity at P2Y2 receptor in human CF/T43 cells, EC50=0.2μM. | 29254895 | |||
| BEA | Function assay | Agonist activity at P2Y2 receptor in BEA cells (unknown origin), EC50=0.2μM. | 29254895 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.237μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.239μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.299μM. | 19419204 | |||
| HEK 293 | Function assay | Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells, EC50=0.59μM. | 15317453 | |||
| 1321N1 | Function assay | Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells, Kb=0.708μM. | 17302398 | |||
| 1321N1 | Function assay | Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=0.85μM. | 23751098 | |||
| 1321N1 | Function assay | 30 mins | Agonist activity at human P2Y1 receptor expressed in human 1321N1 cells assessed as increase of intracellular calcium level after 30 mins using fura-2 AM by fluorescence assay, EC50=0.85μM. | 24846781 | ||
| 1321N1 | Function assay | Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=0.85μM. | 26447940 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=1μM. | 19419204 | |||
| 1321N1 | Function assay | 30 mins | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method, EC50=1μM. | 23075067 | ||
| Sf9 | Function assay | Binding affinity to wild type 6XHis-tagged human JAK2 JH2 domain (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. | 32329617 | |||
| Sf9 | Function assay | Binding affinity to 6XHis-tagged human JAK2 JH2 domain V617F mutant (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. | 32329617 | |||
| 1321N1 | Function assay | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor, EC50=1.5μM. | 11985476 | |||
| Sf9 | Function assay | Binding affinity to recombinant human biotinylated N-terminal GST-tagged autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay, Kd=2.8μM. | 28109791 | |||
| 1321N1 | Function assay | 30 mins | Agonist activity at GFP tagged-human P2Y11 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=3.3μM. | 21090681 | ||
| 1321N1 | Function assay | Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=6.7μM. | 23751098 | |||
| 1321N1 | Function assay | Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=6.7μM. | 26447940 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=11.7μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11, EC50=17.3μM. | 11985476 | |||
| 1321N1 | Function assay | Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells | 17302398 | |||
| MDCK | Function assay | 10 uM | Induction of intracellular calcium level in MDCK cells at 10 uM by Fura-2 in calcium free medium in presence of 10 uM U73343 inactive analogue of U73122 phospholipase C inhibitor | 23163425 | ||
| THLP1 | Function assay | Agonist activity at NLRP3 in human THLP1-null cells assessed as induction of LPS-induced IL-1beta secretion by HEK-Blue reporter cell based assay | 28829599 | |||
| HEK293 | Function assay | 1 uM | Agonist activity at ALX/FPR2 (unknown origin) expressed in HEK293 cells co-expressing Galphaq assessed as induction of intracellular calcium accumulation at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay | 30419493 | ||
| HEK293 | Function assay | 1 uM | Induction of intracellular calcium accumulation in HEK293 cells at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay | 30419493 | ||
| BL21(DE3) | Function assay | Activity of Bacillus subtilis N-terminal His-tagged ANT(6) expressed in Escherichia coli BL21(DE3) cells assessed as adenylated product by Michaelis-Menten kinetics | ChEMBL | |||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 551.14 | Formule | C10H14N5O13P3.2Na |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 987-65-5 | SDF downloaden | Opslag van stamoplossingen |
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| Synoniemen | Adenosine-Triphosphate disodium, Adenosine 5'-triphosphate | Smiles | C1=NC(=C2C(=N1)N(C=N2)C3C(C(C(O3)COP(=O)(O)OP(=O)([O-])OP(=O)(O)[O-])O)O)N.[Na+].[Na+] | ||
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In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
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In vivo |
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Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)
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 de sectie oplosbaarheid.)
Berekeningsresultaten:
Werkconcentratie: mg/ml;
Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.
Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.
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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.
| In vitro |
ATP release and autocrine feedback through P2Y2 and A3 receptors provide signal amplification, controlling gradient sensing and migration of neutrophils. ATP results in production of reactive oxygen species (ROS), which stimulates the phosphatidylinositol 3-kinase (PI3K) pathway and subsequent Akt and ERK1/2 activation. ATP-dependent ROS production and PI3K activation also stimulate transcription of genes required for an oxidative stress response. ATP-mediated ROS-dependent PI3K is required for activation of caspase-1 and secretion of IL-1beta and IL-18. ATP potently stimulates TNF-alpha release, resulting from TNF-alpha mRNA expression in rat cultured brain microglia. ATP-induced TNF-alpha release is Ca(2+)-dependent, and a sustained Ca(2+) influx correlated with the TNF-alpha release in ATP-stimulated microglia. ATP-induced TNF-alpha release is inhibited by PD 098059, an inhibitor of extracellular signal-regulated protein kinase (ERK) kinase 1 (MEK1), which activates ERK, and also by SB 203580, an inhibitor of p38 mitogen-activated protein kinase. ATP rapidly activates both ERK and p38 even in the absence of extracellular Ca(2+). ATP-induced cytotoxicity is mediated by classical alterations of apoptosis, including membrane blebbing, nuclear condensation, and DNA fragmentation. ATP but not other nucleotides lead to the potent and selective activation of NF-κB in microglial cells through a P2Z receptor-mediated pathway. |
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| In vivo |
ATP regulates microglial branch dynamics in the intact mice brain, and its release from the damaged tissue and surrounding astrocytes mediates a rapid microglial response towards injury. |
Referenties |
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(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT04760860 | Not yet recruiting | Dementia With Lewy Bodies |
Qiang Zhang|University of Iowa |
October 2024 | Phase 1|Phase 2 |
| NCT05590195 | Not yet recruiting | Bacterial Vaginosis|Bacterial Infections|Bacterial Vaginosis | Vaginal | Microbiology|Vaginal Infection |
Jeremy Burton|Deerland Enzymes|Lawson Health Research Institute|St. Joseph''s Health Care London |
May 1 2024 | Phase 3 |
| NCT06167512 | Not yet recruiting | Multi-organ Failure After Severe Trauma |
Assistance Publique - Hôpitaux de Paris |
April 1 2024 | -- |