| 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
|
| 详情描述 |
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。
|
| 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.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| ClinicalTrial |
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| 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
|
[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.
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。