EP3 antagonist 6
EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC50 of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats.
For research use only. We do not sell to patients.
- CAS No.: 499149-94-9
- Formula: C31H37NO4
- Molecular Weight:487.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Biological Activity
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EP3 1.9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.9 nM
Compound: 5
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Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
Antagonist activity at mouse EP3alpha receptor expressed in CHO cells assessed as inhibition of PGE2-induced increase in intracellular calcium level after 1 hr by fluorescence assay in presence of 1% bovine serum albumin
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[PMID: 20385498] |
EP3 antagonist 6 (0.1-1 mg/kg; p.o.) shows an AUC of 1.01 μg·h/mL and a Cmax of 0.33 μg/mL[1].
Pharmacokinetic Analysis in EP3 antagonist 6[1]
| Route | Dose (mg/kg) | AUC (μg·h/mL) | t1/2 (h) | Cltot (mL·min/kg) | Vss (L/kg) | Cmax (μg/mL) | F (%) |
| i.v. | 2.7 | 0.89 | 0.4 | 51.5 | 1.24 | / | / |
| p.o. | 10 | 1.01 | 1.6 | / | / | 0.33 | 31 |