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Chemical Structure : BI-749327
CAS No.: 2361241-23-6
Catalog No.: PC-72565Not For Human Use, Lab Use Only.
BI-749327 (BI 749327) is a potent, selective orally bioavailable TRPC6 antagonist (blocker) with IC50 of 13/19/15 nM for mouse/human/guinea pig TRPC6, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $218 | In stock | |
| 25 mg | $488 | In stock | |
| 100 mg | $1280 | In stock | |
| 250 mg | $1980 | In stock | |
| 1 g | Get quote |
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BI-749327 (BI 749327) is a potent, selective orally bioavailable TRPC6 antagonist (blocker) with IC50 of 13/19/15 nM for mouse/human/guinea pig TRPC6, respectively.
BI-749327 displays 85-and 42-fold selectivity over the most closely related channels, TRPC3 and TRPC7, minimally inhibits TRPC5 (>700-fold selective, >500-fold TRPC6 selectivity versus human TRPM8, TRPV1, TRPA1, and Nav1.5 and >150-fold selectivity against human Kv11.1 (hERG).
BI 749327 suppresses NFAT activation in HEK293T cells expressing wild-type or gain-of-function TRPC6 mutants (P112Q, M132T, R175Q, R895C, and R895L) and blocks associated signaling and expression of prohypertrophic genes in isolated myocytes.
BI 749327 (30 mg/kg/day) improves left heart function, reduces volume/mass ratio, and blunts expression of profibrotic genes and interstitial fibrosis in mice.
BI 749327 dose dependently reduces renal fibrosis and associated gene expression in mice with unilateral ureteral obstruction.
| M.Wt | 442.442 | |
| Formula | C23H21F3N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone |
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1. Zheng Z, et al. Sci Rep. 2022 Feb 22;12(1):3038.
2. Jain PP, et al. Am J Physiol Lung Cell Mol Physiol. 2021 Dec 1;321(6):L1161-L1182.
3. Brian Leei Lin, et al. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161.
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