2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. 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.

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EP3 antagonist 6 Chemical Structure

EP3 antagonist 6 Chemical Structure

CAS No. : 499149-94-9

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EP3 antagonist 6 Related Antibodies

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Description

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[1].

IC50 & Target[1]

EP3

1.9 nM (IC50)

In Vivo

EP3 antagonist 6 (0.1-1 mg/kg; p.o.; Single Dose) is effective in eliciting dose-dependent uterine contraction presentation in pregnant rats[1].
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]

药代动力学分析[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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: pregnant rats [1]
Dosage: 0.1 ; 0.3 ; 1 mg/kg; Single Dose
Administration: p.o.
Result: Showed a dose-dependent inhibition of uterine contractions with 29% inhibition at 0.1 mg/kg, 53% at 0.3 mg/kg, and 98% at 1 mg/kg.
Molecular Weight

487.63

Formula

C31H37NO4
CAS No.
SMILES

CC(C)C[C@H](C1=CC(C)=CC(C)=C1)NC(C2=C(C=CC(COC3=C(C=CC=C3)C)=C2)CCC(O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EP3 antagonist 6 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

EP3 antagonist 6499149-94-9Prostaglandin ReceptorEP3PGE2uterine contractionInhibitorinhibitorinhibit

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EP3 antagonist 6
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