CFTRinh172


Catalog No. size PriceQuantity
M6430-2 2mg solid $116
M6430-10 10mg solid $476

Description

CFTRinh172 is a voltage-independent, selective CFTR chloride channel blocker that alters channel gating.

Product information

CAS Number: 307510-92-5

Molecular Weight: 409.40

Formula: C18H10F3NO3S2

Synonym:

CFTR Inhibitor-172

CFTR Inhibitor 172

CFTR Inhibitor172

CFTR(Inh)-172

CFTR(Inh) 172

CFTR(Inh)172

CFTR Inh-172

CFTR Inh 172

CFTR Inh172

Chemical Name: 4-{[(5Z)-4-Oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl}benzoic acid

Smiles: OC(=O)C1C=CC(/C=C2\SC(=S)N(C3=CC(=CC=C3)C(F)(F)F)C\2=O)=CC=1

InChiKey: JIMHYXZZCWVCMI-ZSOIEALJSA-N

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-

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Inhibition by CFTRinh172 is complete in approximately 10 minutes (t1/2=4 minutes) and is reversed after ishout with t1/2 approximately 5 minutes. CFTRinh172 is nontoxic to FRT cells after 24 hours at concentrations up to 100 μM. CFTRinh172 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 CFTRinh172 (250 μg/kg) in mice reduces by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTRinh172 is nontoxic at high concentrations in mouse models. CFTRinh172 significantly reduces fluid secretion to that in saline control loops, whereas an inactive CFTRinh172 analog does not inhibit fluid secretion.

References:

  1. Matuz-Mares D, Hernández-Vázquez A, Riveros-Rosas H, Guinzberg R, Quesada-López T, Cárabez-Trejo A, Mora O, Piña E. β- Adrenoceptors activate hepatic glutathione efflux through an unreported pathway. Arch Biochem Biophys. 2018 Apr 15;644:47-56. doi: 10.1016/j.abb.2018.02.018. Epub 2018 Feb 26. PubMed PMID: 29496543.
  2. Pehote G, Bodas M, Brucia K, Vij N. Cigarette Smoke Exposure Inhibits Bacterial Killing via TFEB-Mediated Autophagy Impairment and Resulting Phagocytosis Defect. Mediators Inflamm. 2017;2017:3028082. doi: 10.1155/2017/3028082. Epub 2017 Dec 28. PubMed PMID: 29445254; PubMed Central PMCID: PMC5763241.
  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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