For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>CFTR(inh)-172 is an reversibly inhibitor of CFTR short-circuit current in less than 2 minutes in a voltage-independent manner with Ki approximately 300 nM.<br>IC50 value: 300 nM (Ki) [1]<br>Target: CFTR<br>in vitro: CFTR(inh)-172 was nontoxic at high concentrations in cell culture and mouse models. At concentrations fully inhibiting CFTR, CFTR(inh)-172 did not prevent elevation of cellular cAMP or inhibit non-CFTR Cl(-) channels, multidrug resistance protein-1 (MDR-1), ATP-sensitive K(+) channels, or a series of other transporters [1]. Short-circuit current experiments indicated similar CFTR(inh)-172 inhibitory potency (K(i) approximately 0.5 microM) for inhibition of Cl(-) current in wild-type, G551D, and G1349D CFTR; however, K(i) was significantly reduced to 0.2 microM for DeltaF508 CFTR [2].<br>in vivo: A single intraperitoneal injection of CFTR(inh)-172 (250 micro g/kg) in mice reduced by more than 90% cholera toxin-induced fluid secretion in the small intestine over 6 hours [1].</p>
| Catalog Number | I003087 |
| CAS Number | 307510-92-5 |
| Synonyms | 4-[(E)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acid |
| Molecular Formula | C₁₈H₁₀F₃NO₃S₂ |
| Purity | ≥95% |
| Target | CFTR |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20C |
| IC50 | 300 nM (Ki) [1] |
| InChI | InChI=1S/C18H10F3NO3S2/c19-18(20,21)12-2-1-3-13(9-12)22-15(23)14(27-17(22)26)8-10-4-6-11(7-5-10)16(24)25/h1-9H,(H,24,25)/b14-8- |
| InChIKey | JIMHYXZZCWVCMI-ZSOIEALJSA-N |
| SMILES | C1=CC(=CC(=C1)N2C(=O)C(=CC3=CC=C(C=C3)C(=O)O)SC2=S)C(F)(F)F |
| Reference | <p style=/line-height:25px/> |
