research use only
Cat.No.S3003
| Related Targets | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR |
|---|---|
| Other PGES Inhibitors | Yakuchinone A |
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | 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 | ||
| Click to View More Cell Line Experimental Data | ||||||
| Molecular Weight | 352.47 | Formula | C20H32O5 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 363-24-6 | Download SDF | Storage of Stock Solutions | Solutions are unstable. Prepare fresh or purchase small, pre-packaged sizes. Repackage upon receipt. | |
| Synonyms | Dinoprostone | Smiles | CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O | ||
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In vitro |
DMSO
: 70 mg/mL
(198.59 mM)
Ethanol : 70 mg/mL Water : 2.5 mg/mL |
|
In vivo |
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| 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 peritoneal macrophages undergoing phagocytosis of the methacrylate microbeads in rats. |
References |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| 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 |
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