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GSK2193874

Name: GSK2193874
Brand: TargetMol
SKU: T5640
Price: 36 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5640Cas No. 1336960-13-4

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

GSK2193874

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Purity: 99.99%

Catalog No. T5640Cas No. 1336960-13-4

GSK2193874 was identified as a selective, orally active TRPV4 blocker.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$36	In Stock	In Stock
2 mg	$52	In Stock	In Stock
5 mg	$74	In Stock	In Stock
10 mg	$129	In Stock	In Stock
25 mg	$259	In Stock	In Stock
50 mg	$426	In Stock	In Stock
100 mg	$633	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$113	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:99.99%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GSK2193874 was identified as a selective, orally active TRPV4 blocker.
Targets&IC50	TRPV4 (rat):2 nM (IC50), TRPV4 (human):40 nM (IC50)
In vitro	GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents[1,2].
In vivo	In isolated rodent and canine lungs, TRPV4 blockade prevented the increased vascular permeability and resultant pulmonary edema associated with elevated PVP. ?In both acute and chronic HF models, GSK2193874 pretreatment inhibited the formation of pulmonary edema and enhanced arterial oxygenation[2].
Animal Research	Adult male Sprague-Dawley rats (n = 7 to 8 per group) were treated with vehicle (6% Cavitron) or GSK2193874 (30 mg/kg/day) via oral gavage for at least 4 days before osmotic challenges.?Rats underwent acute and chronic hyper- and hypo-osmotic challenges.Sprague-Dawley (control, n = 18) and spontaneously hypertensive rats (n = 11) were implanted with Data Sciences International (DSI) radiotelemetry transmitters.?Rats were dosed with GSK2193874, and data were captured with DSI receivers and analyzed with Microsoft Excel[2].

Chemical Properties

Molecular Weight	691.62
Formula	C₃₇H₃₈BrF₃N₄O
Cas No.	1336960-13-4
Smiles	FC(F)(F)c1cccc(c1)-c1nc2cc(Br)ccc2c(C(=O)NC2(CC2)c2ccccc2)c1CN1CCC(CC1)N1CCCCC1
Relative Density.	1.43 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 81.67 mg/mL (118.09 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (5.78 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	1.4459 mL	7.2294 mL	14.4588 mL	72.2940 mL
5 mM	0.2892 mL	1.4459 mL	2.8918 mL	14.4588 mL
10 mM	0.1446 mL	0.7229 mL	1.4459 mL	7.2294 mL
20 mM	0.0723 mL	0.3615 mL	0.7229 mL	3.6147 mL
50 mM	0.0289 mL	0.1446 mL	0.2892 mL	1.4459 mL
100 mM	0.0145 mL	0.0723 mL	0.1446 mL	0.7229 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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