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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 | 128 € | In Stock | |
2 mg | 177 € | In Stock | |
5 mg | 274 € | In Stock | |
10 mg | 432 € | In Stock | |
25 mg | 629 € | In Stock | |
50 mg | 824 € | In Stock | |
100 mg | 1.102 € | In Stock | |
500 mg | 2.204 € | In Stock | |
1 mL x 10 mM (in DMSO) | 301 € | In Stock |
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 (mouse):13 nM (IC50), TRPC6 (Guinea pig):15 nM (IC50), TRPC6 (human):19 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 | 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 | |||||||||||||||||||||||||||||||
DMSO
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