| Name | BI-749327 |
| 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.) 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.52 mM), Sonication is recommended.
DMSO : 27.8 mg/mL (62.83 mM), Sonication is recommended.
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| Keywords | TRPVChannel | TRPV Channel | TRPChannel | TRP Channel | Transient receptor potential channels | mouse TRPC6 | Inhibitor | inhibit | human TRPC6 | guinea pig TRPC6 | BI-749327 | BI749327 | BI 749327 |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
