CFTR(inh)-172
Cat. No.:YN360580
产品名称: | CFTR(inh)-172 |
CAS No.: | 307510-92-5 |
Chemical Name: | 4-[[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl]-benzoic acid |
Synonyms: | CFTR inhibitor 172 |
分子量: | 409.40 |
分子式: | C₁₈H₁₀F₃NO₃S₂ |
SMILES: | S=C(S/1)N(C2=CC=CC(C(F)(F)F)=C2)C(C1=C\C3=CC=C(C=C3)C(O)=O)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | CFTR(inh)-172 是高效选择性的CFTR通道阻断剂; 在2分钟内可逆地抑制CFTR短路电流的Ki值为300 nM。 |
IC50和靶点: | |
In Vitro: | |
In Vivo: | |
Clinical Trial: | |
Solvent & Solubility: |
Derand, R., Bulteau-Pignoux, L., and Becq, F.The cystic fibrosis mutation G551D alters the non-Michaelis-Menten behavior of the cystic fibrosis transmembrane conductance regulator (CFTR) channel and abolishes the inhibitory genistein binding siteJ. Biol. Chem.277(39),35999-36004(2002)
Ma, T., Thiagarajah, J.R., Yang, H., et al.Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretionJ. Clin. Invest.110(11),1651-1658(2002)
Taddei, A., Folli, C., Zegarra-Moran, O., et al.Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blockerFEBS Lett.558(1-3),52-56(2004)
Sonawane, N.D., Hu, J., Muanprasat, C., et al.Luminally active, nonabsorbable CFTR inhibitors as potential therapy to reduce intestinal fluid loss in choleraFASEB J.20(1),130-132(2006)
Yang, B., Sonawane, N.D., Zhao, D., et al.Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney diseaseJ. Am. Soc. Nephrol.19(7),1300-1310(2008)
Duranton, C., Rubera, I., Cougnon, M., et al.CFTR is involved in the fine tuning of intracellular redox status: Physiological implications in cystic fibrosisAm. J. Pathol.181(4),1367-1377(2012)
l'Hoste, S., Chargui, A., Belfodil, R., et al.CFTR mediates apoptotic volume decrease and cell death by controlling glutathione efflux and ROS production in cultured mice proximal tubulesAm. J. Physiol. Renal Physiol.298(2),F435-F453(2010)
Rubera, I., Duranton, C., Melis, N., et al.Role of CFTR in oxidative stress and suicidal death of renal cells during cisplatin-induced nephrotoxicityCell Death Dis.4(10),e817(2013)