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+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| Concentration | Treated Time | Description | References | |
| Renal proximal cells (PCT cells) | 5 µM | 24 hours | CFTR(inh)-172 prevents cisplatin-induced cell death and apoptosis by modulating the intracellular reactive oxygen species (ROS) balance and glutathione (GSH) concentration. | Cell Death Dis. 2013 Oct 3;4(10):e817. |
| A549 cells | 5 µM | 24 hours | CFTR(inh)-172 does not impair the antitumor activity of cisplatin in A549 cancer cells. | Cell Death Dis. 2013 Oct 3;4(10):e817. |
| Human peripheral blood neutrophils | 0.5, 1, 2.5, 5 µM | 4 hours | CFTR(inh)-172 increased CitH3 protein expression and dsDNA fluorescence staining in a concentration-dependent manner, indicating its promotion of NET formation. | Acta Pharmacol Sin. 2022 Nov;43(11):2848-2861. |
| FRT cells | 20 µM | Inhibit CFTR channel activity and reverse the increase in Cl- current induced by anthraquinone compounds | Acta Pharmacol Sin. 2011 Jun;32(6):834-9. |
| Administration | Dosage | Frequency | Description | References | ||
| Rats | Cisplatin-induced nephrotoxicity model | Intraperitoneal injection | 1 mg/kg | Single dose, 30 minutes before cisplatin injection | CFTR(inh)-172 pretreatment significantly prevented cisplatin-induced nephrotoxicity, improved renal function, and reduced oxidative stress. | Cell Death Dis. 2013 Oct 3;4(10):e817. |
| Mice | Wild-type C57BL/6J mice | Intravenous injection | 2 mg/kg | 24 hours | CFTR(inh)-172 increased neutrophil [Cl?]i and dsDNA release, indicating its promotion of NET formation in vivo. | Acta Pharmacol Sin. 2022 Nov;43(11):2848-2861. |
| SD rats | Closed colonic loop model | Intraperitoneal injection | 40 µmol/L | Single dose, lasted for 6 hours | Inhibit fluid accumulation in the colon induced by rhein | Acta Pharmacol Sin. 2011 Jun;32(6):834-9. |
| 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 |
|
| CAS号 | 307510-92-5 |
| 分子式 | C18H10F3NO3S2 |
| 分子量 | 409.4 |
| SMILES Code | O=C1N(C2=CC=CC(C(F)(F)F)=C2)C(S/C1=C\C3=CC=C(C(O)=O)C=C3)=S |
| MDL No. | MFCD01164609 |
| 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 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
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