CFTR(inh)-172
Based on 25 publication(s) in Google Scholar
CFTR(inh)-172 is a potent and selective blocker of the CFTR chloride channel; reversibly inhibits CFTR short-circuit current in less than 2 minutes with a Ki of 300 nM.
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- Pureté: 99.80%
- CAS No.: 307510-92-5
- Formule: C18H10F3NO3S2
- Masse moléculaire:409.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CFTR(inh)-172
More- Cell Stem Cell. 2019 Sep 5;25(3):373-387.e9. [Abstract]
- Nat Commun. 2026 Jun 9. [Abstract]
- Nat Commun. 2026 Jan 8;17(1):1253. [Abstract]
- J Clin Invest. 2024 Jan 16;134(2):e171249. [Abstract]
- Adv Sci (Weinh). 2025 Aug 21:e01661. [Abstract]
- Carbohydr Polym. 2025 Dec 10;376:124810.
- PLoS Biol. 2021 Feb 16;19(2):e3001090. [Abstract]
- J Ethnopharmacol. 2026 Mar 25:359:121101. [Abstract]
- Mol Diagn Ther. 2025 Sep 13. [Abstract]
- ACS Appl Bio Mater. 2024 Dec 16;7(12):8489-8502. [Abstract]
- Int J Mol Sci. 2022 Feb 23;23(5):2442. [Abstract]
- Am J Physiol Cell Physiol. 2025 Nov 1;329(5):C1550-C1559. [Abstract]
- Am J Physiol Cell Physiol. 2025 Oct 1;329(4):C1130-C1138. [Abstract]
- Am J Physiol Cell Physiol. 2025 Mar 1;328(3):C856-C871. [Abstract]
- ACS Omega. 2023 Nov 25;8(48):45606-45615. [Abstract]
- Neuropharmacology. 2025 Dec 14:286:110808. [Abstract]
- J Physiol. 2025 May;603(9):2619-2632. [Abstract]
- iScience. 2025 Feb 1;28(3):111942. [Abstract]
- Biomedicines. 2025 Jan 1;13(1):82. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2025 Aug 13. [Abstract]
- Andrology. 2025 Feb;13(2):371-381. [Abstract]
- Physiol Rep. 2026 Jun;14(11):e70975. [Abstract]
- Research Square Preprint. 2023 Dec 22.
- bioRxiv. 2023 Jul 31.
- J Pers Med. 2023 Jan 1;13(1):102. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
Activité biologique
Ki: 300 nM (CFTR)[1]
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[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 307510-92-5
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Appearance Solid
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Masse moléculaire 409.40
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Formule C18H10F3NO3S2
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Color Light yellow to yellow
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SMILES
S=C(S/1)N(C2=CC=CC(C(F)(F)F)=C2)C(C1=C\C3=CC=C(C=C3)C(O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (25)
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Journal Impact Factor
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Most Recent
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Cell Stem Cell
Generation of Human PSC-Derived Kidney Organoids with Patterned Nephron Segments and a De Novo Vascular Network. [Abstract]2019 Sep 5;25(3):373-387.e9. PMID: 31303547
CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: Cell Stem Cell. 2019 Sep 5;25(3):373-387.e9. [Abstract]
Representative bright-field images of ARPKD kidney organoids treated with various concentrations of CFTRinh172 (50 µM to 100 µM) in the absence or presence of 10 μM FSK for 3 days (Day 28 to 31). Scale bars, 500 μm.
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Nat Commun
2026 Jun 9. PMID: 42265113 -
Nat Commun
2026 Jan 8;17(1):1253. PMID: 41507162
CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jan 8;17(1):1253. [Abstract]
Procedure to determine the effect of CaCCinh-A01 (A01; 3 mg/kg), an ANO1 inhibitor and CFTRinh-172 (172; 1 mg/kg, i.p., 30 min prior to the administration of DAB, every 12 h for 24 h), a CFTR inhibitor on DAB-induced laxative effect.
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J Clin Invest
Mg2+ supplementation treats secretory diarrhea in mice by activating calcium-sensing receptor in intestinal epithelial cells. [Abstract]2024 Jan 16;134(2):e171249. PMID: 37962961
CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jan 16;134(2):e171249. [Abstract]
Isc traces in T84 cells showing the forskolin concentration response and CFTRinh-172 (10 μM) inhibition following 20 minutes of pretreatment with the indicated concentrations of CaCl2 or 30 μM cinacalcet (left). Summary of changes in Isc (Δ Isc) from the experiments (right).
CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jan 16;134(2):e171249. [Abstract]
Δ Isc induced by CFTRinh-172 in the presence of different Ca2+ concentrations and cinacalcet. n = 3–6 per group. Data indicate the mean ± SEM.
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Adv Sci (Weinh)
2025 Aug 21:e01661. PMID: 40841925
CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 21:e01661. [Abstract]
Bright‐field images of cystic kidney organoids treated with chloride channel inhibitors CFTR inhibitor‐172 (CFTRinh‐172, 50-100 μM) for 24 h. The cystic kidney organoids were generated by treating organoids with forskolin 30 µm for 48 h.
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PLoS Biol
2021 Feb 16;19(2):e3001090. PMID: 33591965 -
J Ethnopharmacol
Shenling Baizhu powder alleviates pyrotinib-induced diarrhea via CFTR-activated chloride secretion. [Abstract]2026 Mar 25:359:121101. PMID: 41461327 -
Mol Diagn Ther
Personalized Medicine in Cystic Fibrosis: Characterization of Eight Rare CFTR Variants in Intestinal Organoids and Cellular Models. [Abstract]2025 Sep 13. PMID: 40944809 -
ACS Appl Bio Mater
Differential Effects of Confinement on the Dynamics of Normal and Tumor-Derived Pancreatic Ductal Organoids. [Abstract]2024 Dec 16;7(12):8489-8502. PMID: 39576883 -
Int J Mol Sci
2022 Feb 23;23(5):2442. PMID: 35269585 -
Am J Physiol Cell Physiol
Zinc inhibits cAMP-induced Cl- secretion in intestinal epithelial cells via calcium-sensing receptor. [Abstract]2025 Nov 1;329(5):C1550-C1559. PMID: 41051948 -
Am J Physiol Cell Physiol
(R)-vanzacaftor potentiates BKCa channels in the absence of CFTR correction or potentiation. [Abstract]2025 Oct 1;329(4):C1130-C1138. PMID: 40920663 -
Am J Physiol Cell Physiol
Modeling ocular surface ion and water transport by generation of lipid- and mucin-producing human meibomian gland and conjunctival epithelial cells. [Abstract]2025 Mar 1;328(3):C856-C871. PMID: 39870373 -
ACS Omega
2023 Nov 25;8(48):45606-45615. PMID: 38075767 -
Neuropharmacology
Cftr nominates a novel therapeutic target for Alzheimer's disease: Evidence from integrative omics and in vitro validation. [Abstract]2025 Dec 14:286:110808. PMID: 41401902 -
J Physiol
2025 May;603(9):2619-2632. PMID: 40047394 -
iScience
Global functional genomics reveals GRK5 as a cystic fibrosis therapeutic target synergistic with current modulators. [Abstract]2025 Feb 1;28(3):111942. PMID: 40040803 -
Biomedicines
2025 Jan 1;13(1):82. PMID: 39857666 -
Am J Physiol Lung Cell Mol Physiol
Effect of elexacaftor and bamocaftor on the metabolic and thermal stability of the F508del-CFTR protein in human airway epithelial cells. [Abstract]2025 Aug 13. PMID: 40803756 -
Andrology
Cellular mechanism underlying leptin-induced anion secretion of rat epididymal epithelial cells. [Abstract]2025 Feb;13(2):371-381. PMID: 38778669 -
Physiol Rep
Monosodium glutamate-mediated Ca2+-dependent intestinal epithelial ion transports in health and IBS-D in male mice. [Abstract]2026 Jun;14(11):e70975. PMID: 42281391 -
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J Pers Med
2023 Jan 1;13(1):102. PMID: 36675763
Solvant et solubilité
DMSO : 50 mg/mL (122.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.11 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
CFTR(inh)-172 is diluted in DMSO as a 10 mM stock solution and diluted with appropriate medium. Fischer rat thyroid (FRT) cells coexpressing human wild-type CFTR and the halide indicator YFP-H148Q are generated. Cell toxicity is assayed by the dihydrorhodamine method at 24 hours after cell incubation with 0–1,000 μM inhibitor CFTR(inh)-172[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Animal toxicity is assessed by measurement of serum chemistries and hematology in mice at 5 days after daily intraperitoneal injections with 0-1,000 μg/kg CFTR(inh)-172[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (761 KB)
- English - EN (761 KB)
- Français - FR (761 KB)
- Deutsch - DE (761 KB)
- Norwegian - NO (761 KB)
- Español - ES (761 KB)
- Swedish - SV (761 KB)
- Italian - IT (761 KB)
- Korean - KR (761 KB)
- Portuguese - PT (761 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ma T, et al. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J Clin Invest. 2002 Dec;110(11):1651-8. [Content Brief]
[2]. Taddei A, et al. Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett. 2004 Jan 30;558(1-3):52-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4426 mL | 12.2130 mL | 24.4260 mL | 61.0650 mL |
| 5 mM | 0.4885 mL | 2.4426 mL | 4.8852 mL | 12.2130 mL | |
| 10 mM | 0.2443 mL | 1.2213 mL | 2.4426 mL | 6.1065 mL | |
| 15 mM | 0.1628 mL | 0.8142 mL | 1.6284 mL | 4.0710 mL | |
| 20 mM | 0.1221 mL | 0.6106 mL | 1.2213 mL | 3.0532 mL | |
| 25 mM | 0.0977 mL | 0.4885 mL | 0.9770 mL | 2.4426 mL | |
| 30 mM | 0.0814 mL | 0.4071 mL | 0.8142 mL | 2.0355 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6106 mL | 1.5266 mL | |
| 50 mM | 0.0489 mL | 0.2443 mL | 0.4885 mL | 1.2213 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4071 mL | 1.0177 mL | |
| 80 mM | 0.0305 mL | 0.1527 mL | 0.3053 mL | 0.7633 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2443 mL | 0.6106 mL |
CFTR(inh)-172 Related Classifications
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