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CAS No. : 459856-18-9
MCE 国际站:Pexacerfont
产品活性:Pexacerfont 是一种选择性的促肾上腺皮质激素释放因子 (CRF1) 受体拮抗剂,作用于人 CRF1 受体,IC50 为 6.1±0.6 nM。
研究领域:GPCR/G Protein
作用靶点:CRFR
In Vitro: Pexacerfont demonstrates a potent and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward human CRF1 receptor and has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors.
In Vivo: Pexacerfont (BMS-562086) is active in rats (1-10 mg/kg, orally) in the defensive withdrawal and elevated plus maze models of anxiety. After the intravenous bolus dose, the plasma Pexacerfont concentrations exhibited a multiexponential decline in rats, dogs, and chimpanzees. The CLp of Pexacerfont was higher in rats (17.9 mL/kg per min) and dogs (11.6 mL/kg per min) than in chimpanzees (2.0 mL/kg per min). Assuming the value of CLp of Pexacerfont approximates the value of CLb in these three species, Pexacerfont has an estimated hepatic extraction ratio of 0.32, 0.38, and 0.08 in rats, dogs, and chimpanzees, respectively (calculated by dividing CLp by respective hepatic blood flow, 55.2, 30.9, and 25.5 mL/kg per min for rats, dogs, and chimpanzees). The assumption that CLb is equal to CLp is reasonable at least in rats, where the blood to plasma concentration ratio of BMS-562086-equivalent radioactivity was 0.95 at 1 h postdose.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Endocrinology Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | Antisauvagine-30 TFA | Cortagine | CRF, bovine | Urocortin, rat | Sauvagine TFA | Urocortin III, mouse | [DPro5] Corticotropin Releasing Factor, human, rat | α-Helical CRF(9-41) TFA | Verucerfont | (Tyr0)-Urocortin, rat | R121919 | DMP 696 | CP 316311 | Urocortin III (human) | Urocortin II, human | CP 376395 | Emicerfont | (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) | NBI-27914 | CRF(6-33)(human) TFA | Urotensin I TFA | K41498 | Antalarmin | a-Helical Corticotropin Releasing Factor (12-41) | Urocortin, human
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