aladdin 阿拉丁 G414121 GLPG1837 1654725-02-6 98%

中文名：GLPG1837

英文名：GLPG1837

纯度：≥98%

货号：G414121

Cas号：1654725-02-6

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

GLPG1837 GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.

Targets

CFTR(F508del) ; CFTR(G551D) 3 nM(EC50); 339 nM(EC50)

In vitro

GLPG1837 has an attractive in vitro ADME profile, showing low Clint,unb in both microsomal and hepatocytes stability assays, good permeability, and no off-target inhibition of CYPs and the hERG channel.

In vivo

The pharmacokinetic profile of GLPG1837 is attractive, showing a low Cl,unb and good F% in both rat and dog. The CL (L/h/kg) of GLPG1837 after intravenous injection of 1 mg/kg dose are 1.92 and 0.32 in rats and dogs, respectively. T_1/2 is 1.84 h in rats while 3 h in dogs. After 5 mg/kg p.o, the oral availability of GLPG1837 in rat is 67%. In dogs, F%>100.

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