GLPG1837
目录号: PL01870 纯度: ≥99%
CAS No. :1654725-02-6
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中文名称
GLPG1837
英文名称
GLPG1837
英文别名
GLPG1837;N-(3-carbamoyl-5,5,7,7-tetramethyl-4,7-dihydro-5H-thieno[2,3-c]pyran-2-yl)-1H-pyrazole-3-carboxamide;GLGP1837;GLPG 1837;BCP23611;BDBM50246760;s8698;AK00778999;Q29207083;CC1(C)Cc2c(sc(NC(=O)c3ccn[nH]3)c2C(N)=O)C(C)(C)O1;LJP
Cas No.
1654725-02-6
分子式
C16H20N4O3S
分子量
348.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GLPG1837 是一种有效的,可逆的 CFTR 增强剂,对 CFTR 的 突变体 F508del 和 G551D 的 EC50 值分别为 3 nM 和 339 nM。
生物活性
GLPG1837 is a potent and reversible CFTR potentiator, with EC 50 s of 3 nM and 339 nM for F508del and G551D CFTR, respectively.
性状
Solid
IC50 & Target[1][2]
EC50: 3 nM (F508del CFTR), 339 nM (G551D CFTR)
体外研究(In Vitro)
GLPG1837 is a potent CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. GLPG1837 increases the conductivity of the G551D CFTR channel with obtained potency of 181 nM. GLPG1837 is reversible CFTR potentiator, with a the apparent affinity within a range of 0.2~2 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : ≥ 250 mg/mL (717.52 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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