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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 /CFTR(inh)-172 {[allProObj[0].p_purity_real_show]}

货号:A285038 同义名: CFTR Inhibitor-172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172

CFTR(inh)-172是一种可逆抑制剂,能够在不到 2 分钟内通过电压独立方式抑制 CFTR 短路电流,Ki 值约为 300 nM。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
CFTR(inh)-172 化学结构 CAS号:307510-92-5
CFTR(inh)-172 化学结构
CAS号:307510-92-5
CFTR(inh)-172 3D分子结构
CAS号:307510-92-5
CFTR(inh)-172 化学结构 CAS号:307510-92-5
CFTR(inh)-172 3D分子结构 CAS号:307510-92-5
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CFTR(inh)-172 纯度/质量文件 产品仅供科研

货号:A285038 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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产品名称 CFTR 其他靶点 纯度
Ataluren 98%
Lumacaftor ++++

F508del-CFTR, EC50: 0.1 μM

98%
CFTR(inh)-172 +++

CFTR, Ki: 300 nM

99%+
GlyH-101 +

CFTR, Ki: 4.3 μM

99%+
IOWH-032 ++

CFTR, IC50: 1.01 μM

99%+
Tezacaftor 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

CFTR(inh)-172 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].

CFTR(inh)-172 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

CFTR(inh)-172 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.

CFTR(inh)-172 实验方案

计算器
存储液制备 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

CFTR(inh)-172 技术信息

CAS号307510-92-5
分子式C18H10F3NO3S2
分子量 409.402
别名 CFTR Inhibitor-172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172;CFTRinh-172
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方
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