alleen voor onderzoeksdoeleinden
Cat.nr.: S3003
Chemische structuur
| Gerelateerde doelwitten | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR |
|---|---|
| Overig PGES Inhibitoren | Yakuchinone A |
| Cellijnen | Assaytype | Concentratie | Incubatietijd | Formulering | Activiteitsbeschrijving | PMID |
|---|---|---|---|---|---|---|
| HeLa | Function assay | TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, Km = 0.094 μM. | 7754369 | |||
| HeLa | Function assay | TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, K1/2 = 0.1 μM. | 8787677 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OCT2-expressing S2 cells, Km = 0.0289 μM. | 11907186 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OAT4-expressing S2 cells, Km = 0.154 μM. | 11907186 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OAT3-expressing S2 cells, Km = 0.345 μM. | 11907186 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OCT1-expressing S2 cells, Km = 0.657 μM. | 11907186 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OAT2-expressing S2 cells, Km = 0.713 μM. | 11907186 | |||
| S2 | Function assay | TP_TRANSPORTER: uptake in OAT1-expressing S2 cells, Km = 0.97 μM. | 11907186 | |||
| HEK293 | Function assay | Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cells, IC50 = 0.0007 μM. | 12643927 | |||
| HEK293 | Function assay | EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor, EC50 = 0.003 μM. | 12643927 | |||
| Sf9 | Function assay | TP_TRANSPORTER: uptake (vesicle) in membrane vesicles from MRP4-expressing Sf9 cells, Km = 3.4 μM. | 12835412 | |||
| HEK293 | Function assay | Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells, Ki = 0.00033 μM. | 17531488 | |||
| HEK293 | Function assay | Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells, Ki = 0.00079 μM. | 17531488 | |||
| HEK293 | Function assay | Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells, Ki = 0.0049 μM. | 17531488 | |||
| HEK293 | Function assay | Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells, Ki = 0.0091 μM. | 17531488 | |||
| HEK293 | Function assay | Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0002 μM. | 19250823 | |||
| HEK293 | Function assay | Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0007 μM. | 19250823 | |||
| HEK293 | Function assay | Inhibition of rat EP4 receptor expressed in HEK293 cells, IC50 = 0.0021 μM. | 19250823 | |||
| HEK293 | Function assay | Inhibition of rat EP2 receptor expressed in HEK293 cells, IC50 = 0.0052 μM. | 19250823 | |||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0031 μM. | 22119471 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.005 μM. | 22119471 | ||
| CHO | Function assay | 20 mins | Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting, Ki = 0.006 μM. | 22119471 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.022 μM. | 22119471 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.0031 μM. | 22386979 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.005 μM. | 22386979 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.006 μM. | 22386979 | ||
| CHO | Function assay | 60 mins | Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.022 μM. | 22386979 | ||
| CHEM1 | Function assay | 2 hrs | Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, Ki = 0.00045 μM. | 23403082 | ||
| CHEM1 | Function assay | 2 hrs | Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, IC50 = 0.0011 μM. | 23403082 | ||
| CHO | Function assay | 100 nM | Activity at recombinant EP1 receptor (unknown origin) expressed in CHO cells co-expressing Gq protein at 100 nM by electrical cell substrate impedance sensing system | 25701254 | ||
| CHO | Function assay | 100 nM | Activity at recombinant EP4 receptor (unknown origin) expressed in CHO cells co-expressing Gs protein at 100 nM by electrical cell substrate impedance sensing system | 25701254 | ||
| CHO | Function assay | 100 nM | Activity at recombinant EP3 receptor (unknown origin) expressed in CHO cells co-expressing Gi protein at 100 nM by electrical cell substrate impedance sensing system | 25701254 | ||
| CHO | Function assay | 30 mins | Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0019 μM. | 26985320 | ||
| CHO | Function assay | Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0025 μM. | 26985320 | |||
| CHO | Function assay | Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0037 μM. | 26985320 | |||
| CHO | Function assay | 30 mins | Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0075 μM. | 26985320 | ||
| Chem1 | Function assay | Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.25 μM. | 26985320 | |||
| HEK293 | Function assay | 90 mins | Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay, EC50 = 0.346 μM. | 26985320 | ||
| CHO | Function assay | 30 mins | Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.347 μM. | 26985320 | ||
| HEK293 | Function assay | Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells, IC50 = 0.0026 μM. | 26988801 | |||
| HEK293 | Function assay | 120 mins | Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.00055 μM. | 27876250 | ||
| HEK293 | Function assay | 120 mins | Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.0026 μM. | 27876250 | ||
| Klik om meer experimentele gegevens over cellijnen te bekijken | ||||||
| Molecuulgewicht | 352.47 | Formule | C20H32O5 |
Opslag (vanaf de datum van ontvangst) | |
|---|---|---|---|---|---|
| CAS-nr. | 363-24-6 | SDF downloaden | Opslag van stamoplossingen | Oplossingen zijn instabiel. Bereid ze vers of koop kleine, voorverpakte formaten. Herverpakken na ontvangst. | |
| Synoniemen | Dinoprostone | Smiles | CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O | ||
|
In vitro |
DMSO
: 70 mg/mL
(198.59 mM)
Ethanol : 70 mg/mL Water : 2.5 mg/mL |
|
In vivo |
|||||
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 |
PGE2 acts via EP4 receptors on osteoclasts during the progression of OA and OA-related pain. |
|---|---|
| In vivo |
PGE2 (0.3 μg/k, i.p.) significantly reduces the number of peritoneab macrophages undergoing phagocytosis of the methacrybate microbeads in rats. |
Referenties |
(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)
| NCT-nummer | Werving | Aandoeningen | Sponsor/medewerkers | Startdatum | Fasen |
|---|---|---|---|---|---|
| NCT06129604 | Recruiting | Colorectal Carcinoma (CRC)|Endometrial Carcinoma (EC) |
University of Oklahoma |
April 3 2024 | Phase 2 |
| NCT06307678 | Completed | Periapical; Infection |
Ataturk University |
July 7 2023 | Not Applicable |
| NCT06190132 | Completed | Uremic Pruritus in Hemodialysis Patients |
Ain Shams University |
April 1 2023 | Not Applicable |