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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 |
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). |
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.) improves left heart function, reduces volume/mass ratio, and blunts expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload. BI-749327 dose-dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction. BI-749327 (3-30 mg/kg; p.o.) has a long terminal half-life (t1/2 8.5-13.5 hours) for mice. |
Molecular Weight | 442.43 |
Formula | C23H21F3N4O2 |
Cas No. | 2361241-23-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 31.25 mg/mL (70.63 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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