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. T1/2 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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关键字： D80376 ; ABBV-974; GLPG-1837 ; ABBV974 ; ABBV 974
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