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BI-749327

Name: BI-749327
Brand: TargetMol
SKU: T10537
Price: 135 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰Excellent

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

🥰Excellent

Purity: 99.84%

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 Size	Price	USA Warehouse	Global Warehouse
1 mg	$135	In Stock	In Stock
2 mg	$187	In Stock	In Stock
5 mg	$289	In Stock	In Stock
10 mg	$455	In Stock	In Stock
25 mg	$663	In Stock	In Stock
50 mg	$868	In Stock	In Stock
100 mg	$1,160	In Stock	In Stock
500 mg	$2,320	-	In Stock
1 mL x 10 mM (in DMSO)	$317	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Batch Information

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Purity:99.84%

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COA LCMS HNMR

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 (Guinea pig):15 nM (IC50), TRPC6 (human):19 nM (IC50), TRPC6 (mouse):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.) 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 Weight	442.43
Formula	C₂₃H₂₁F₃N₄O₂
Cas No.	2361241-23-6
Smiles	Nc1ccc(nn1)C1CCN(CC1)C(=O)c1ccc(Oc2ccc(cc2)C(F)(F)F)cc1
Relative Density.	1.334 g/cm3 (Predicted)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 31.25 mg/mL (70.63 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.52 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2602 mL	11.3012 mL	22.6024 mL	113.0122 mL
5 mM	0.4520 mL	2.2602 mL	4.5205 mL	22.6024 mL
10 mM	0.2260 mL	1.1301 mL	2.2602 mL	11.3012 mL
20 mM	0.1130 mL	0.5651 mL	1.1301 mL	5.6506 mL
50 mM	0.0452 mL	0.2260 mL	0.4520 mL	2.2602 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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