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CFTRinh-172

现货
Catalog No.
B1435
CFTR抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 700.00
现货
10mg
¥ 1,030.00
现货
50mg
¥ 3,290.00
现货

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Background

Ki: 0.3 to 5 μM for channel opening

The cystic fibrosis (CF) transmembrane regulator (CFTR) is a cAMP-activated Cl channel expressed in epithelial cells of the lung, intestine, pancreas, and other tissues, where it facilitates transepithelial fluid transport. CFTRinh-172 is a highly potent and selective CFTR inhibitor.

In vitro: CFTRinh-172 could reversibly inhibit CFTR short-circuit current in less than 2 minutes in a voltage-independent manner. Moreover, at concentrations fully inhibiting CFTR, CFTRinh-172 did not prevent elevation of cellular cAMP or inhibit non-CFTR Cl–channels, multidrug resistance protein-1, ATP-sensitive K+ channels, or a series of other transporters [2].

In vivo: A single ip injection of CFTRinh-172 (250 μg/kg) in mice reduced by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTRinh-172 may be useful in developing large-animal models of cystic fibrosis and reducing intestinal fluid loss in cholera and other secretory diarrheas [3].

Clinical trial: Up to now, CFTRinh-172 is still in the preclinical development stage.

Reference:
[1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS.  Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.

Chemical Properties

StorageStore at -20°C
M.Wt409.4
Cas No.307510-92-5
FormulaC18H10F3NO3S2
Solubility≥40.9mg/mL in DMSO
Chemical Name4-[(E)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acid
SDFDownload SDF
Canonical SMILESC1=CC(=CC(=C1)N2C(=O)C(=CC3=CC=C(C=C3)C(=O)O)SC2=S)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

表达人类野生型CFTR的Fischer大鼠甲状腺细胞

溶解方法

在DMSO中的溶解度> 20.5mg/mL。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

1 mM

应用

CFTRinh-172在表达CFTR的上皮细胞中抑制cAMP/黄酮刺激的Cl-转运。

动物实验[1]:

动物模型

小鼠

剂量

腹腔注射,250μg/ kg

应用

在霍乱毒素输注之前单次施用CFTRinh-172有效地防止了毒素处理引起的肠道中的液体积聚。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.

质量控制

化学结构

CFTRinh-172