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BI-749327

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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).

BI-749327

BI-749327

🥰Excellent
Purity: 99.68%
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).
Pack SizePriceAvailabilityQuantity
1 mg128 €In Stock
2 mg177 €In Stock
5 mg274 €In Stock
10 mg432 €In Stock
25 mg629 €In Stock
50 mg824 €In Stock
100 mg1.102 €In Stock
500 mg2.204 €In Stock
1 mL x 10 mM (in DMSO)301 €In Stock
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Purity:99.68%
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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).
Targets&IC50
TRPC6 (mouse):13 nM (IC50), TRPC6 (Guinea pig):15 nM (IC50), TRPC6 (human):19 nM (IC50)
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.) enhances left heart function, lowers volume/mass ratio, and mitigates profibrotic gene expression and interstitial fibrosis in mice under sustained pressure overload. Additionally, BI-749327 dose-dependently decreases renal fibrosis and related gene expression in mice with unilateral ureteral obstruction. BI-749327 (3-30 mg/kg; p.o.) exhibits a long terminal half-life (t1/2 8.5-13.5 hours) in mice.
Chemical Properties
Molecular Weight442.43
FormulaC23H21F3N4O2
Cas No.2361241-23-6
SmilesNc1ccc(nn1)C1CCN(CC1)C(=O)c1ccc(Oc2ccc(cc2)C(F)(F)F)cc1
Relative Density.1.334 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 31.25 mg/mL (70.63 mM), Sonication is recommended.
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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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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