BAY-1316957

BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC 50 of 15.3 nM for human EP4-R . BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research In Vitro BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male adult Sprague Dawley rats (220-265 g) injected with 16,16-dimethyl prostaglandin E2 (dmPGE2) Dosage: 0.2 mg/kg, 1 mg/kg, 5 mg/kg Administration: Oral administration; once Result: Significantly reduced paw withdrawal thresholds in dmPGE2 pain model. Form:Solid IC50& Target:human EP4-R 15.3 nM (IC 50 )

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