BI-749327
Based on 16 publication(s) in Google Scholar
BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 2361241-23-6
- Formula: C23H21F3N4O2
- Molecular Weight:442.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BI-749327
More- Biomed Pharmacother. 2023 May:161:114480. [Abstract]
- Cell Rep. 2025 Nov 25;44(11):116543. [Abstract]
- Cell Rep. 2023 Oct 31;42(11):113347. [Abstract]
- Am J Physiol Cell Physiol. 2022 Oct 1;323(4):C959-C973. [Abstract]
- Exp Neurol. 2023 May:363:114350. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2022 Nov 1;1868(11):166505. [Abstract]
- Cell Calcium. 2023 Jun:112:102738. [Abstract]
- Biomedicines. 2022 Jul 1;10(7):1574. [Abstract]
- Sci Rep. 2022 Feb 22;12(1):3038. [Abstract]
- Function (Oxf). 2024 Jun 10:zqae030. [Abstract]
- Am J Physiol Lung Cell Mol Physiol. 2021 Dec 1;321(6):L1161-L1182. [Abstract]
- Behav Brain Funct. 2025 Jul 22;21(1):23. [Abstract]
- Toxicon. 2026 Jun 15:276:109072. [Abstract]
- Transfus Med. 2023 Jun;33(3):232-243. [Abstract]
- bioRxiv. 2026 Jan 2:2026.01.01.697223. [Abstract]
- bioRxiv. 2024 Mar 11.
Biological Activity
IC50: 13 nM (mouse TRPC6), 19 nM (human TRPC6), 15 nM (guinea pig TRPC6)[1]
BI-749327 suppresses NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants and blocks associated signaling and expression of prohypertrophic genes in isolated myocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BI-749327 dose dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction[1].
BI-749327 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice[1]
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Dosage:30 mg/kg/day
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Administration:Oral gavage
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Result:Improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload.
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Animal Model:CD-1 mice[1]
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Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration
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Result:t1/2 8.5-13.5 hours
Chemical Information
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CAS No. 2361241-23-6
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Appearance Solid
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Molecular Weight 442.43
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Formula C23H21F3N4O2
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Color White to off-white
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SMILES
NC1=NN=C(C2CCN(C(C3=CC=C(OC4=CC=C(C(F)(F)F)C=C4)C=C3)=O)CC2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Biomed Pharmacother
Interruption of TRPC6-NFATC1 signaling inhibits NADPH oxidase 4 and VSMCs phenotypic switch in intracranial aneurysm. [Abstract]2023 May:161:114480. PMID: 37002575 -
Cell Rep
2025 Nov 25;44(11):116543. PMID: 41206865 -
Cell Rep
The calcium channel TRPC6 promotes chemotherapy-induced persistence by regulating integrin α6 mRNA splicing. [Abstract]2023 Oct 31;42(11):113347. PMID: 37910503 -
Am J Physiol Cell Physiol
Mechanosensitive cation currents through TRPC6 and Piezo1 channels in human pulmonary arterial endothelial cells. [Abstract]2022 Oct 1;323(4):C959-C973. PMID: 35968892 -
Exp Neurol
Trpc6 knockout improves behavioral dysfunction and reduces Aβ production by inhibiting CN-NFAT1 signaling in T2DM mice. [Abstract]2023 May:363:114350. PMID: 36791875 -
Biochim Biophys Acta Mol Basis Dis
TRPC6 N338S is a gain-of-function mutant identified in patient with doxorubicin-induced cardiotoxicity. [Abstract]2022 Nov 1;1868(11):166505. PMID: 35882306 -
Cell Calcium
High-throughput assessment identifying major platelet Ca2+ entry pathways via tyrosine kinase-linked and G protein-coupled receptors. [Abstract]2023 Jun:112:102738. PMID: 37060673 -
Biomedicines
Klotho Modulates Pro-Fibrotic Activities in Human Atrial Fibroblasts through Inhibition of Phospholipase C Signaling and Suppression of Store-Operated Calcium Entry. [Abstract]2022 Jul 1;10(7):1574. PMID: 35884879 -
Sci Rep
2022 Feb 22;12(1):3038. PMID: 35194063 -
Function (Oxf)
2024 Jun 10:zqae030. PMID: 38984988 -
Am J Physiol Lung Cell Mol Physiol
2021 Dec 1;321(6):L1161-L1182. PMID: 34704831 -
Behav Brain Funct
Chronic lipopolysaccharide exposure promotes cognitive impairments by activating TRPC6-AIM2 inflammasome signaling and the regulation of ginsenoside Rg1 in Trpc6-/- mice. [Abstract]2025 Jul 22;21(1):23. PMID: 40696361 -
Toxicon
Transient receptor potential canonical 6 is critical for chronic lipopolysaccharide exposure-induced pulmonary injury and fibrosis. [Abstract]2026 Jun 15:276:109072. PMID: 41850440 -
Transfus Med
2023 Jun;33(3):232-243. PMID: 36746770 -
bioRxiv
Functional Evaluation of TRPC6 Missense Variants in Cancer Patients via Molecular Docking Analysis Compared with Patch Clamp Electrophysiology. [Abstract]2026 Jan 2:2026.01.01.697223. PMID: 41509376 -
Solvent & Solubility
DMSO : 31.25 mg/mL (70.63 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 2.08 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2602 mL | 11.3012 mL | 22.6024 mL | 56.5061 mL |
| 5 mM | 0.4520 mL | 2.2602 mL | 4.5205 mL | 11.3012 mL | |
| 10 mM | 0.2260 mL | 1.1301 mL | 2.2602 mL | 5.6506 mL | |
| 15 mM | 0.1507 mL | 0.7534 mL | 1.5068 mL | 3.7671 mL | |
| 20 mM | 0.1130 mL | 0.5651 mL | 1.1301 mL | 2.8253 mL | |
| 25 mM | 0.0904 mL | 0.4520 mL | 0.9041 mL | 2.2602 mL | |
| 30 mM | 0.0753 mL | 0.3767 mL | 0.7534 mL | 1.8835 mL | |
| 40 mM | 0.0565 mL | 0.2825 mL | 0.5651 mL | 1.4127 mL | |
| 50 mM | 0.0452 mL | 0.2260 mL | 0.4520 mL | 1.1301 mL | |
| 60 mM | 0.0377 mL | 0.1884 mL | 0.3767 mL | 0.9418 mL |
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