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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-BI-749327
BI-749327

Chemical Structure : BI-749327

CAS No.: 2361241-23-6

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BI-749327 (BI 749327)

货号: 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.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 442.442
分子式 C23H21F3N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(4-(6-aminopyridazin-3-yl)piperidin-1-yl)(4-(4-(trifluoromethyl)phenoxy)phenyl)methanone

参考文献

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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