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GSK205

🥰Excellent
Catalog No. T11480Cas No. 1263068-83-2

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

GSK205

GSK205

🥰Excellent
Purity: 99.46%
Catalog No. T11480Cas No. 1263068-83-2
GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.
Pack SizePriceAvailabilityQuantity
1 mg$64In Stock
5 mg$156In Stock
10 mg$272In Stock
25 mg$587In Stock
50 mg$993In Stock
100 mg$1,730In Stock
1 mL x 10 mM (in DMSO)$165In Stock
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Purity:99.46%
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Product Introduction

Bioactivity
Description
GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.
Targets&IC50
TRPV4:4.19  μM
In vitro
In T3-F442A adipocytes, GSK205 (5 μM; 4 days) resulted in increased expression of thermogenic genes and was accompanied by a decrease in the proinflammatory gene program[1].
In vivo
In male C57BL/6J mice on a high-fat diet, GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days) caused a reduced expression of proinflammatory chemokines, macrophage markers, and Tnfa in EPI fat. It also significantly improved glucose tolerance in diet-induced obese (DIO) mice[1].
Chemical Properties
Molecular Weight481.45
FormulaC24H25BrN4S
Cas No.1263068-83-2
SmilesBr.CN(CCc1ccc(Nc2ncc(s2)-c2cccnc2)cc1)Cc1ccccc1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (207.71 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0771 mL10.3853 mL20.7706 mL103.8529 mL
5 mM0.4154 mL2.0771 mL4.1541 mL20.7706 mL
10 mM0.2077 mL1.0385 mL2.0771 mL10.3853 mL
20 mM0.1039 mL0.5193 mL1.0385 mL5.1926 mL
50 mM0.0415 mL0.2077 mL0.4154 mL2.0771 mL
100 mM0.0208 mL0.1039 mL0.2077 mL1.0385 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | 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 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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