CFTRinh172


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

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

 

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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