产品描述: | CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM. |
靶点: |
Ki: 300 nM (CFTR);CFTR;Autophagy |
体内研究: |
A single intraperitoneal injection of CFTR(inh)-172 (250 μg/kg) in mice reduces by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTR(inh)-172 is nontoxic at high concentrations in mouse models. CFTRinh-172 significantly reduces fluid secretion to that in saline control loops, whereas an inactive CFTRinh-172 analog does not inhibit fluid secretion |
参考文献: |
1. Ma T, 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. 2. Taddei A, et al. Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett. 2004 Jan 30;558(1-3):52-6. |
溶解性: |
DMSO : 50 mg/mL (122.13 mM; Need ultrasonic) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.443 ml |
12.213 ml |
24.426 ml |
5 mM |
0.489 ml |
2.443 ml |
4.885 ml |
10 mM |
0.244 ml |
1.221 ml |
2.443 ml |
50 mM |
0.049 ml |
0.244 ml |
0.489 ml |
|
注意: |
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