货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T96354-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T96354-1ml ￥648.00 现货	5 5	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T96354-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

CFTR 活化剂;CFTR Activators;;InformationGLPG1837 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.TargetsCFTR(F508del) ; CFTR(G551D) 3 nM(EC50); 339 nM(EC50)In vitroGLPG1837 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 vivoThe 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.

靶点：

EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR)

参考文献：

1. Van der Plas SE, et al. Discovery of N-(3-Carbamoyl-5,5,7,7-tetramethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-2-yl)-lH-pyrazole-5-carboxamide (GLPG1837), a Novel Potentiator Which Can Open Class III Mutant Cystic Fibrosis Transmembrane Conductance Regulator (
2. Yeh HI, et al. A common mechanism for CFTR potentiators. J Gen Physiol. 2017 Dec 4;149(12):1105-1118.

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.87 ml	14.35 ml	28.701 ml
5 mM	0.574 ml	2.87 ml	5.74 ml
10 mM	0.287 ml	1.435 ml	2.87 ml
50 mM	0.057 ml	0.287 ml	0.574 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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