CFTRinh-172 (Synonyms: CFTR(inh)172, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172) |
Catalog No.GC14421 |
CFTRinh-172는 CFTR 염화물 채널의 강력하고 선택적인 차단제입니다. 300nM의 Ki로 2분 이내에 CFTR 단락 전류를 가역적으로 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 307510-92-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Fischer rat thyroid cells expressing human wild-type CFTR |
Preparation method |
The solubility of this compound in DMSO is >20.5mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
1 mM |
Applications |
CFTRinh-172 inhibited cAMP/flavone-stimulated Cl– transport in epithelial cells expressing CFTR. |
Animal experiment [1]: | |
Animal models |
Mice |
Dosage form |
250 μg/kg intraperitoneally |
Application |
A single administration of CFTRinh-172 prior to cholera toxin infusion effectively prevented fluid accumulation in the toxin-treated intestinal loops. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8. |
Ki: 0.3 to 5 μM for channel opening
The cystic fibrosis (CF) transmembrane regulator (CFTR) is a cAMP-activated Cl channel expressed in epithelial cells of the lung, intestine, pancreas, and other tissues, where it facilitates transepithelial fluid transport. CFTRinh-172 is a highly potent and selective CFTR inhibitor.
In vitro: CFTRinh-172 could reversibly inhibit CFTR short-circuit current in less than 2 minutes in a voltage-independent manner. Moreover, at concentrations fully inhibiting CFTR, CFTRinh-172 did not prevent elevation of cellular cAMP or inhibit non-CFTR Cl–channels, multidrug resistance protein-1, ATP-sensitive K+ channels, or a series of other transporters [2].
In vivo: A single ip injection of CFTRinh-172 (250 μg/kg) in mice reduced by more than 90% cholera toxin–induced fluid secretion in the small intestine over 6 hours. CFTRinh-172 may be useful in developing large-animal models of cystic fibrosis and reducing intestinal fluid loss in cholera and other secretory diarrheas [3].
Clinical trial: Up to now, CFTRinh-172 is still in the preclinical development stage.
Reference:
[1] Ma T, Thiagarajah JR, Yang H, Sonawane ND, Folli C, Galietta LJ, Verkman AS. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8.
Cas No. | 307510-92-5 | SDF | |
Synonyms | CFTR(inh)172, Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172 | ||
Chemical Name | 4-[(E)-[4-oxo-2-sulfanylidene-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]methyl]benzoic acid | ||
Canonical SMILES | C1=CC(=CC(=C1)N2C(=O)C(=CC3=CC=C(C=C3)C(=O)O)SC2=S)C(F)(F)F | ||
Formula | C18H10F3NO3S2 | M.Wt | 409.4 |
Solubility | ≥ 40.9mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4426 mL | 12.213 mL | 24.426 mL |
5 mM | 0.4885 mL | 2.4426 mL | 4.8852 mL |
10 mM | 0.2443 mL | 1.2213 mL | 2.4426 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 29 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *