GLPG1837
作者：齐岳
发布时间：2023-09-08
09:07:41
点击数：
产品名称：GLPG1837
产品描述：
| 产品描述 | GLPG1837 is an effective CFTR potentiator, with EC50s of 3 nM and 339 nM for F508del and G551D CFTR, respectively. |
| 靶点活性 | F508del CFTR:3 nM (EC50), G551D CFTR:339 nM (EC50) |
| 体外活性 | GLPG1837 increases the conductivity of the G551D CFTR channel with the obtained potency of 181 nM[1]. GLPG1837 is reversible CFTR potentiator, with the apparent affinity within a range of 0.2～2 μM[2]. |
| 细胞实验 | CFBe41o- cells are cultured in Eagle's Minimal Essential Medium (MEM) supplemented with 10% fetal bovine serum (FBS), 1% penicillin/streptomycin, 1% l-glutamine, and 500 μg/mL hygromycin B. The cells are grown on culture flasks coated with 0.01% bovine serum albumin (BSA), 30 μg/mL Purecol, and 0.001% human fibronectin. CFBe41o- cells are transduced with adenoviruses containing F508del CFTR and YFP (H148Q/I152L/F47L). HEK293 cells are cultured in Dulbecco's Modified Eagle Medium (DMEM) supplemented with 10% FBS and 1% penicillin/streptomycin. HEK293 cells are transfected with plasmids containing G551D, G178R, S549N, R117H, CFTR, and YFP (H148Q/I152L/F47L). Directly after transfection, the HEK293 cells are seeded in black 96-well plates coated with poly-d-lysine at a density of 70000 cells per well. The next day, cells are incubated for 24 h at 27°C (CFBE41o?) or 37°C (HEK293). Then cells are treated for 10 min with 10 μM forskolin and the desired concentration of potentiator at room temperature. |
| 别名 | ABBV-974 |
| 分子量 | 348.42 |
| 分子式 | C16H20N4O3S |
| CAS No. | 1654725-02-6 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 60 mg/mL
H2O: Insoluble
Ethanol: 5 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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