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BI-749327

BI-749327
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Purity:99.74%
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BI-749327

Catalog No. T10537Cas No. 2361241-23-6
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).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePriceAvailabilityQuantity
1 mg$135In Stock
2 mg$187In Stock
5 mg$289In Stock
10 mg$455In Stock
25 mg$663In Stock
50 mg$868In Stock
100 mg$1,160In Stock
500 mg$2,320In Stock
1 mL x 10 mM (in DMSO)$317In Stock
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Product Introduction

Bioactivity
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.) 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 (3-30 mg/kg; p.o.) has a long terminal half-life (t1/2 8.5-13.5 hours) for mice.
Chemical Properties
Molecular Weight442.43
FormulaC23H21F3N4O2
Cas No.2361241-23-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 31.25 mg/mL (70.63 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2602 mL11.3012 mL22.6024 mL113.0122 mL
5 mM0.4520 mL2.2602 mL4.5205 mL22.6024 mL
10 mM0.2260 mL1.1301 mL2.2602 mL11.3012 mL
20 mM0.1130 mL0.5651 mL1.1301 mL5.6506 mL
50 mM0.0452 mL0.2260 mL0.4520 mL2.2602 mL

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