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BI-749327
🥰Excellent
Catalog No. T10537Cas No. 2361241-23-6
BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6).
BI-749327
🥰Excellent
Purity: 99.68%
Catalog No. T10537Cas No. 2361241-23-6
BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $135 | In Stock | |
| 2 mg | $187 | In Stock | |
| 5 mg | $289 | In Stock | |
| 10 mg | $455 | In Stock | |
| 25 mg | $663 | In Stock | |
| 50 mg | $868 | In Stock | |
| 100 mg | $1,160 | In Stock | |
| 500 mg | $2,320 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $317 | In Stock |
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CitedSelect Batch
Purity:99.68%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6). |
| Targets&IC50 | TRPC6 (Guinea pig):15 nM (IC50), TRPC6 (human):19 nM (IC50), TRPC6 (mouse):13 nM (IC50) |
| In vitro | BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7. 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. |
| In vivo | BI-749327 (30 mg/kg/day; i.g.) enhances left heart function, lowers volume/mass ratio, and mitigates profibrotic gene expression and interstitial fibrosis in mice under sustained pressure overload. Additionally, BI-749327 dose-dependently decreases renal fibrosis and related gene expression in mice with unilateral ureteral obstruction. BI-749327 (3-30 mg/kg; p.o.) exhibits a long terminal half-life (t1/2 8.5-13.5 hours) in mice. |
| Molecular Weight | 442.43 |
| Formula | C23H21F3N4O2 |
| Cas No. | 2361241-23-6 |
| Smiles | Nc1ccc(nn1)C1CCN(CC1)C(=O)c1ccc(Oc2ccc(cc2)C(F)(F)F)cc1 |
| Relative Density. | 1.334 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 31.25 mg/mL (70.63 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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