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CAS No. : 1613264-40-6
MCE 国际站:BAY-1316957
产品活性: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 具有出色的活性分子代谢和药代动力学特性,并可用于子宫内膜异位的研究。
研究领域:GPCR/G Protein
作用靶点:Prostaglandin Receptor
In Vitro: BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay.
In Vivo: BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model.
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.
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