2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. EP3 antagonist 6

EP3 antagonist 6 (compound 5) 是一种口服有效的、选择性的 EP3 receptor 拮抗剂，IC50 值为 1.9 nM。EP3 antagonist 6 可抑制 PGE2 (HY-101952) 诱导的妊娠大鼠子宫收缩。

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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 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

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)

体内研究
(In Vivo)

EP3 antagonist 6 (0.1-1 mg/kg; p.o.; 单剂量) 在怀孕的老鼠中能有效的引起剂量依赖性的子宫收缩[1]。
EP3 antagonist 6 (10 mg/kg; p.o.; 单剂量) AUC 为1.01 μg · h/mL，Cmax 为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

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.
分子量

487.63

Formula

C31H37NO4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

EP3 antagonist 6 相关分类

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Keywords:

EP3 antagonist 6499149-94-9Prostaglandin ReceptorEP3PGE2uterine contractionInhibitorinhibitorinhibit

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