Cat. No.: HY-16671

CFTR(inh)-172

25 Cited Publications

Customer Review

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 K_i of 300 nM.

For research use only. We do not sell to patients.

Purity: 99.80%
CAS No.: 307510-92-5
Formula: C₁₈H₁₀F₃NO₃S₂
Molecular Weight:409.40

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CFTR(inh)-172 Chemical Structure

CAS No.: 307510-92-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (25)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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 K_i of 300 nM.

IC₅₀ & Target

Ki: 300 nM (CFTR)^[1]

In Vitro

Inhibition by CFTR(inh)-172 is complete in approximately 10 minutes (t_1/2=4 minutes) and is reversed after ishout with t_1/2 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 K_i=0.6 μM. This effect is due to increased mean channel closed time without changing mean channel open time. The K_i values for inhibition of Cl^- current in wild-type, G551D, and G1349D CFTR are about 0.5 μM; however, K_i 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.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 307510-92-5
Appearance Solid
Molecular Weight 409.40
Formula C₁₈H₁₀F₃NO₃S₂
Color Light yellow to yellow
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
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (25)

All Cell Imaging/StainingIn Vivo Efficacy StudyBio/Physico-chemical Assay

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Journal Impact Factor

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.
Nat Commun

Inhibition of the QPCT-PDIA4 axis rescues ΔF508 and N1303K CFTR in cystic fibrosis. [Abstract]

2026 Jun 9. PMID: 42265113
Nat Commun

Noncanonical calcium-independent TRPM4 activation governs intestinal fluid homeostasis. [Abstract]

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.
Adv Sci (Weinh)

Developmental Hypoxia Enhances Kidney Organoid Complexity and Maturity. [Abstract]

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.
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]

I^sc 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 I^sc) from the experiments (right).

CFTR(inh)-172 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Jan 16;134(2):e171249. [Abstract]

Δ I^sc induced by CFTRinh-172 in the presence of different Ca2+ concentrations and cinacalcet. n = 3–6 per group. Data indicate the mean ± SEM.
Carbohydr Polym

2025 Dec 10;376:124810.
PLoS Biol

The protease corin regulates electrolyte homeostasis in eccrine sweat glands. [Abstract]

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
Int J Mol Sci

Proximity Profiling of the CFTR Interaction Landscape in Response to Orkambi. [Abstract]

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 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
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
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
J Physiol

The apical mucus layer alters the pharmacological properties of the airway epitheliumy. [Abstract]

2025 May;603(9):2619-2632. PMID: 40047394
ACS Omega

Synthesis and Evaluation of Ivacaftor Derivatives with Reduced Lipophilicity. [Abstract]

2023 Nov 25;8(48):45606-45615. PMID: 38075767
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

Rescue of Mutant CFTR Channel Activity by Investigational Co-Potentiator Therapy. [Abstract]

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]

2024 May 22. 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
Research Square Preprint

2023 Dec 22.
bioRxiv

2023 Jul 31.
J Pers Med

Additive Potentiation of R334W-CFTR Function by Novel Small Molecules. [Abstract]

2023 Jan 1;13(1):102. PMID: 36675763

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4426 mL

12.2130 mL

24.4260 mL

5 mM

0.4885 mL

2.4426 mL

4.8852 mL

10 mM

0.2443 mL

1.2213 mL

2.4426 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protocol

Cell Assay^[1]

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.

Animal Administration^[1]

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

CFTR(inh)-172

25 Cited Publications

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CFTR(inh)-172

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Covalent Screening Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CFTR(inh)-172

Biological Activity

Chemical Information

Publications (25)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CFTR(inh)-172

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Covalent Screening Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Bioactive Compound Library Max

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) CFTR(inh)-172

Biological Activity

Chemical Information

Publications (25)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

CFTR(inh)-172 Related Classifications

HY-16671 Related Classifications