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CFTR(inh)-172

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Chemical Structure| 307510-92-5 同义名 : CFTR Inhibitor-172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172;CFTRinh-172
CAS号 : 307510-92-5
货号 : A285038
分子式 : C18H10F3NO3S2
纯度 : 99%+
分子量 : 409.402
MDL号 : MFCD01164609
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(122.13 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CFTR

    CFTR, Ki:300 nM
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 KI 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 Kd 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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.43mL

4.89mL

2.44mL
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.