Pexacerfont

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服活性的 CRF1 受体拮抗剂，IC50 为 6.1 nM，选择性是 CRF 结合蛋白和生物胺受体的 1,000 倍以上。

A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors; demonstrates oral effectivity in rat models of anxiety, possesses good pharmacokinetic profile in vivo.Irritable Bowel Syndrome Phase 2 Discontinued.

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.

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.

BMS-562086 | BMS562086 | DPC-A69448

GPCR/G Protein

CRF Receptor

CRF Receptor

Other Indications

Irritable Bowel Syndrome

459856-18-9

340.431

C18H24N6O

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (146.88 mM)

CC[C@H](NC1=NC(C)=NC2=C(C3=CC=C(OC)N=C3C)C(C)=NN21)C

8-(6-Methoxy-2-methyl-3-pyridinyl)-2,7-dimethyl-N-[(1R)-1-methylpropyl]pyrazolo[1,5-a]-1,3,5-triazin-4-amine

(-20℃)

With Ice Pack

≥ 2 years