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Merck
CN

219671

GlyH-101

≥97% (HPLC), solid, CFTR inhibitor, Calbiochem®

别名:

CFTR抑制剂II,GlyH-101

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关于此项目

经验公式(希尔记法):
C19H15Br2N3O3
化学文摘社编号:
分子量:
493.15
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.28
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze
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产品名称

CFTR抑制剂II,GlyH-101, CFTR Inhibitor II, GlyH-101, CAS 328541-79-3, is a cell-permeable potent, selective and reversible open-channel blocker of CFTR (Ki = 4.3 µM in CFTR-expressing FRT cells).

Quality Level

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

yellow

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

Brc1c(c(cc(c1O)\C=N\NC(=O)CNc2cc3c(cc2)cccc3)Br)O

InChI

1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+

InChI key

RMBDLOATEPYBSI-NUGSKGIGSA-N

General description

一种可渗透细胞的甘氨酰腙化合物,以中等速度作为CFTR的有效,选择性和可逆的开放通道阻滞剂(<1 min; 95% inhibition at 50 µM; Ki = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl- currents, and is effective in nasal and intestinal epithelia in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 219675)。

Biochem/physiol Actions

在表达CFTR的FRT细胞中为4.3 µM,用于顶膜氯离子电流
主要靶标
CFTR
产物不与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:以50 µM时抑制95%

Preparation Note

复溶后,等分并冷冻保存(-20°C)。储备液在-20°C条件下可稳定保存3个月。

Other Notes

Sonawane, N.D., et al. 2006.FASEB J.20, 130.
Muanprasat, C., et al. 2004.J. Gen.Physiol.124, 125.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:标准处理(A)


存储类别

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



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全球贸易项目编号

货号GTIN
219671-5MG07790788048747