BI-749327

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BI-749327 是一种高选择性、口服生物可利用的 TRPC6 拮抗剂（对于小鼠、人类和豚鼠 TRPC6，IC50 分别为 13 nM、19 nM 和 15 nM）。

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).

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.

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 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.). Animal Model:C57BL/6J miceDosage:30 mg/kg/day Administration:Oral gavage Result:Improved left heart function, reduced volume/mass ratio, and blunted expression of profibrotic genes and interstitial fibrosis in mice subjected to sustained pressure overload.Animal Model:CD-1 mice Dosage:3 mg/kg, 10 mg/kg, 30 mg/kg Administration:Oral administrationResult:t1/2 8.5-13.5 hours

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

mouse TRPC6|human TRPC6|guinea pig TRPC6

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2361241-23-6

442.43

C23H21F3N4O2

>98% (HPLC)

DMSO:31.25 mg/mL (70.63 mM; Need ultrasonic)

NC1=NN=C(C2CCN(C(C3=CC=C(OC4=CC=C(C(F)(F)F)C=C4)C=C3)=O)CC2)C=C1

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(-20℃)

With Ice Pack

≥ 2 years