Powder: -20°C for 3 years | In solvent: -80°C for 2 years
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 135.00 | |
5 mg | In stock | $ 289.00 | |
10 mg | In stock | $ 455.00 | |
25 mg | In stock | $ 753.00 | |
50 mg | In stock | $ 1,060.00 | |
100 mg | In stock | $ 1,430.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 317.00 |
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 | guinea pig TRPC6:15 nM (IC50), human TRPC6:19 nM (IC50), mouse TRPC6:13 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.) 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 31.25 mg/mL (70.63 mM), Need ultrasonic
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
bottom
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.
BI-749327 2361241-23-6 Membrane transporter/Ion channel TRP/TRPV Channel BI749327 Inhibitor inhibit Transient receptor potential channels BI 749327 TRP Channel inhibitor