GLPG1837CAS号： 1654725-02-6分子式： C16H20N4O3S分子量： 348.42描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
GLPG1837 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. |
| 纯度 |
＞98%
|
| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 别名 |
GLPG-1837；GLPG 1837；ABBV-974； ABBV 974； ABBV974
|
| 外观 |
powder
|
| 可溶性/溶解性 |
DMSO：69 mg/mL (198.04 mM)
Ethanol :5 mg/mL (14.35 mM) |
| 生物活性 | |
| 靶点 |
CFTR(F508del),CFTR(G551D)
|
| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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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分子结构图
