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BI-749327

Catalog No. T10537 CAS 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 products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

BI-749327, CAS 2361241-23-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 135.00
5 mg	In stock	$ 289.00
10 mg	In stock	$ 455.00
25 mg	In stock	$ 753.00
50 mg	In stock	$ 1,060.00
100 mg	In stock	$ 1,430.00
1 mL * 10 mM (in DMSO)	In stock	$ 317.00

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Purity: 99.74%

Biological Description

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Storage & Solubility Information

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	guinea pig TRPC6:15 nM (IC50), human TRPC6:19 nM (IC50), mouse TRPC6:13 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.) 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.

Molecular Weight	442.43
Formula	C23H21F3N4O2
CAS No.	2361241-23-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

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

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Lin B L, et al. In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Orally Active Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max Neuronal Signaling Compound Library Bioactive Compound Library Ion Channel Inhibitor Library

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Related compounds with same targets

TRPM4-IN-2 EIPA hydrochloride GSK3395879 D-GsMTx4 TFA Dihydromorin GSK2798745 JYL 1421 Capsiate

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

BI-749327 2361241-23-6 Membrane transporter/Ion channel TRP/TRPV Channel BI749327 Inhibitor inhibit Transient receptor potential channels BI 749327 TRP Channel inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.