BI-749327 is a potent, high selectivity and orally bioavailable TRPC6 antagonist, with IC50s of 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6, respectively. BI-749327 is 85-fold more selective for mouse TRPC6 than TRPC3 and 42-fold versus TRPC7.

Product information

CAS Number: 2361241-23-6

Molecular Weight: 442.43

Formula: C23H21F3N4O2

Chemical Name: 6-(1-{4-[4-(trifluoromethyl)phenoxy]benzoyl}piperidin-4-yl)pyridazin-3-amine

Smiles: NC1C=CC(=NN=1)C1CCN(CC1)C(=O)C1C=CC(=CC=1)OC1C=CC(=CC=1)C(F)(F)F

InChiKey: RGYMFGHHIDRCBN-UHFFFAOYSA-N

InChi: InChI=1S/C23H21F3N4O2/c24-23(25,26)17-3-7-19(8-4-17)32-18-5-1-16(2-6-18)22(31)30-13-11-15(12-14-30)20-9-10-21(27)29-28-20/h1-10,15H,11-14H2,(H2,27,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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 has long terminal half-life (t1/2 8.5-13.5 hours) for mice (3-30 mg/kg; p.o.).

Products are for research use only. Not for human use.