Description
Cas:307510-92-5
Product Information:
CFTRinh172 is a voltage-independent, selective CFTR chloride channel blocker that alters channel gating.
Chemical Formula: C18H10F3NO3S2
Exact Mass: 409.0054
Molecular Weight: 409.39
Elemental Analysis: C, 52.81; H, 2.46; F, 13.92; N, 3.42; O, 11.72; S, 15.66
Synonym:
CFTR Inh-172
CFTR Inh 172
CFTR Inh172
CFTR(Inh)-172
CFTR(Inh) 172
CFTR(Inh)172
CFTR Inhibitor-172
CFTR Inhibitor 172
CFTR Inhibitor172
Chemical Name: 4-{[(5Z)-4-Oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl}benzoic acid
InChi Key:
JIMHYXZZCWVCMI-ZSOIEALJSA-N
InChi Code: 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-
Smiles Code:
O=C(O)C1=CC=C(/C=C(SC(N2C3=CC=CC(C(F)(F)F)=C3)=S)/C2=O)C=C1
Technical Data:
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
In Vitro:
Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t1/2=4 minutes) and is reversed after ishout with t1/2 approximately 5 minutes. CFTRinh-172 is nontoxic to FRT cells after 24 hours at concentrations up to 100 μM[1]. CFTR(inh)-172 does not alter CFTR unitary conductance (8 pS), but reduces open probability by > 90% with Ki=0.6 μM. This effect is due to increased mean channel closed time without changing mean channel open time. The Ki values for inhibition of Cl- current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, Ki is significantly reduced to 0.2 μM for vF508 CFTR.
In Vivo:
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.
References:
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3. Mroz MS, Lajczak NK, Goggins BJ, Keely S, Keely SJ. The bile acids, deoxycholic acid and ursodeoxycholic acid, regulate colonic epithelial wound healing. Am J Physiol Gastrointest Liver Physiol. 2018 Mar 1;314(3):G378-G387. doi: 10.1152/ajpgi.00435.2016. Epub 2018 Jan 11. PubMed PMID: 29351391.
4. Shi R, Xiao ZT, Zheng YJ, Zhang YL, Xu JW, Huang JH, Zhou WL, Li PB, Su WW. Naringenin Regulates CFTR Activation and Expression in Airway Epithelial Cells. Cell Physiol Biochem. 2017;44(3):1146-1160. doi: 10.1159/000485419. Epub 2017 Nov 27. PubMed PMID: 29179179.
5. Yu B, Jiang Y, Zhang B, Yang H, Ma T. Resveratrol dimer trans-ε-viniferin prevents rotaviral diarrhea in mice by inhibition of the intestinal calcium-activated chloride channel. Pharmacol Res. 2018 Mar;129:453-461. doi: 10.1016/j.phrs.2017.11.016. Epub 2017 Nov 14. PubMed PMID: 29155014.
Products are for research use only. Not for human use.
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