BAY-1316957 是一种有效的，选择性的，具有口服活性的前列腺素 E2 受体亚型 4 (EP4-R) 的拮抗剂，对人 EP4-R 的 IC50 为 15.3 nM。BAY-1316957 具有出色的药物代谢和药代动力学特性，并可用于子宫内膜异位的研究。
货号:ajcx38634
CAS:1613264-40-6
分子式:C27H27N3O3
分子量：441.52
溶解度:DMSO : 100 mg/mL (226.49 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent drug metabolism and pharmacokinetics properties, and can be used for endometriosis research[1].

BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay[1].

BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model[1].The pharmacokinetic parameters of BAY-1316957 (Compound 32) shows a low clearance, long half-life, and high bioavailability (F%=90%) in Wistar rats. Investigation of the metabolic pathways of BAY-1316957 (Compound 32) in human, rat, mouse, dog, and monkey hepatocytes revealed that the formation of the acyl glucuronide was also the common and predominant route of biotransformation, mainly catalyzed by UGT1A1 and to a lesser extent by UGT1A3[1].

[1]. BÄurle S, et al. Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis. J Med Chem. 2019 Mar 14;62(5):2541-2563.

Protocol:

h-EP4 15.3nM(IC50)