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CFTR Activator, Cact-A1-Calbiochem

品牌
Sigma-Aldrich
货号
5.05985
包装型号
规格纯度
参考价格
2417.18 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
CFTR Activator, Cact-A1-Calbiochem
Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1, 5-(( Z)-2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-3-amino-1H-pyrazole-4-carbonitrile, ( Z)-3-(2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-5-amino-1H-pyrazole-4-carbonitrile
Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1, 5-((Z)-2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-3-amino-1H-pyrazole-4-carbonitrile, (Z)-3-(2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-5-amino-1H-pyrazole-4-carbonitrile
产品介绍:

产品说明

一般描述

A non-cytotoxic (30 µM for 48 h in human airway epithelial Calu-3 cultures) aminopyrazolocarbonitrile compound that is shown to activate both wt- and ΔF508-CFTR channel activity in a cAMP-independent, reversible, and CFTRinh-172- (Cat. Nos. 219670 & 219674) blockable (IC50 & IC100 = 0.37 & 30 µM, respectively, against 30 µM Cact using Fisher rat thyroid/FRT cells with wt-CFTR) manner, without affecting CaCC (Calcium-activated chloride channel) function or cellular levels of Ca2+ and cAMP. The maximum activation inducible by Cact-A1 (ECmax = 13 to 30 µM in Cl- current induction using in Fisher rat thyroid/FRT and primary human bronchial epithelial/HBE cells) is comparable to that achievable via cAMP stimulation by Forskolin treatment (ECmax = 20 µM; Cat. Nos. 344270 & 34427082), which cannot be further enhanced by Forskolin co-treatment in cells expressing wt-CFTR, although additive effects are seen when Cact-A1 and Forskoklin are applied at suboptimal concentrations to cells with wt-CFTR or when the two drugs are applied at respective ECmax to cells with surface ΔF508-CFTR. Neither Cact-A1 nor Forskolin alone (at 30 µM; and 20 µM;, respectively) can effectively activate FRT with surface G551D-CFTR or primary HNPE (human nasal polyp epithelial) cells with surface G551D/Y1092X-CFTR, while Cact-A1-Forskolin co-treatment results in synergistic activation and maximally achievable activation is reported with a three-drug co-treatment using Cact-A1, Forskolin, and VX-770 (at 30, 20, and 10 µM, respectively).
A cell-permeable, non-toxic aminopyrazolocarbonitrile compound that acts as a potent, selective, reversible and cAMP-independent activator of CFTR-dependent Cl- channel in airway epithelial cells (EC50 = 1.6 µM in CFTR-expressing Fisher rat thyroid cells). Also shown to activate ΔF508-CFTR in primary CF-HBE cell cultures (EC50 = 3.5 µM). Reported to directly bind to the same site as CFTRinh-172 (>Cat. No. 219670, >Cat. No. 219674). Does neither elevate intracellular cAMP levels nor appear to have any requirement for cAMP agonist, such as forskolin (Cat. No. 344270, Cat. No. 344282). Shown to additively potentiate the G551D-CFTR Cl- current activated by forskolin with CFTR potentiator, VX-770. Exerts no effect on either Ca2+-activated Cl- channel (TMEM16A) or intracellular Ca2+ levels.

生化/生理作用

Cell permeable: yes
Reversible: yes
Primary Target
CFTR

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Namkung, W., et al. 2013. Mol. Pharmacol.84, 384.

法律信息

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

基本信息

经验(实验)分子式C16H13N5O
分子量291.31

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色light yellow
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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