|3-[(3-三氟甲基)苯基]-5-[(4-羧基苯基)亚甲基]-2-硫代-4-噻唑烷酮|CsnPharm

CAS No.: 307510-92-5

CFTR(inh)-172/5-[（4-羧基苯基）亚甲基]-2-硫氧-3- [（3-三氟甲基）苯基-4-噻唑烷酮 Catalog No. CSN19349

Synonyms: CFTR inhibitor 172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172;CFTR Inh-172

CFTR (inh)-172 is an reversibly inhibitor of CFTR short-circuit current in less than 2 minutes in a voltage-independent manner with Ki ~300 nM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CFTR

Ki:300nM
描述The cystic fibrosis transmembrane conductance regulator (CFTR) protein is cAMP-activated epithelial Cl^- channel required for fluid secretion in the intestine and airways. CFTR(inh)-172 reversibly inhibited CFTR short-circuit current in a voltage-independent manner with a K_I of approximately 300nM. CFTR(inh)-172 significantly inhibited CFTR at dosages of 0.3-0.6μM. In CFTR-expressing FRT cells, treatment with CFTR(inh)-172 led to a dose-dependent inhibition of short-circuit current with a K_d value of approximately 300nM. CFTR(inh)-172 at 5μM did not block Ca²⁺-activated Cl^- secretion in polarized human bronchial epithelial cell or volume-activated Cl^- currents in FRT cells. A single intraperitoneal injection of CFTR(inh)-172 (250μg/kg) in mice before cholera toxin infusion prevented fluid accumulation in the toxin-treated intestinal loops^[3].
作用机制CFTR(inh)-172 is a potent blocker of the CFTR Cl^- channel that reversibly inhibits CFTR short-circuit current^[3].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
rat FRT cells	-	Function assay	-	Inhibition of human wild type CFTR expressed in rat FRT cells assessed as chloride current by short-circuit current measurements, IC50=0.38 μM	18691893

参考文献

[1] Lu M, Ding C. CFTR-mediated Cl(-) transport in the acinar and duct cells of rabbit lacrimal gland. Curr Eye Res. 2012 Aug;37(8):671-7.
[2] Ma T, Thiagarajah JR, et al. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.
[3] Ma T, Thiagarajah JR, Yang H, et al. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002;110(11):1651-1658.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4426 mL
- 12.2129 mL
- 24.4259 mL
- 5 mM
- 0.4885 mL
- 2.4426 mL
- 4.8852 mL
- 10 mM
- 0.2443 mL
- 1.2213 mL
- 2.4426 mL

技术信息

CAS号

307510-92-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H10F3NO3S2

运输

蓝冰

分子量

409.40

别名

CFTR inhibitor 172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172;CFTR Inh-172;CFTR(Inh)-172

溶解度

DMSO	81.0 mg/mL (197.8 mM)
Water	Insoluble
Ethanol	Insoluble

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CFTR(inh)-172/5-[（4-羧基苯基）亚甲基]-2-硫氧-3- [（3-三氟甲基）苯基-4-噻唑烷酮 Catalog No. CSN19349

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