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616522 TRPV4 Antagonist III, GSK205 - Calbiochem

TRPV4 Antagonist III, GSK205 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine, HBr

616522
  
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Overview

Replacement Information
Description
Overview

This product has been discontinued.



A pyridinylthiazolamine compound that is shown to inhibit TRPV4-mediated Ca2+ influx induced by 1 µM 4α-PDD (Cat. No. 524394) or Hypo-osmotic stress in primary porcine articular chondrocytes (10 µM GSK205 pretreatment). Also reported to effectively block Ca2+ mobilization induced by 100 nM TRPV4 agonist GSK101 in murine 3T3-F442A adipocytes in vitro and improve glucose tolerance (1 g/kg glucose via i.p.) in high fat diet-induced obese mice (10 mg GSK205/kg/12 h; i.p.) in vivo.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number616522
Brand Family Calbiochem®
SynonymsN-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine, HBr
References
ReferencesYe, L., et al. 2012. Cell 151, 96.
Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.
Product Information
FormOrange powder
Hill FormulaC₂₄H₂₄N₄S • HBr
Chemical formulaC₂₄H₂₄N₄S • HBr
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetTRPV4 channel
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
616522 0

Documentation

References

Reference overview
Ye, L., et al. 2012. Cell 151, 96.
Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision27-September-2013 JSW
SynonymsN-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine, HBr
DescriptionA pyridinylthiazolamine compound that is shown to inhibit TRPV4-mediated Ca2+ influx induced by 1 µM 4α-PDD (Cat. No. 524394; cell population with intracellular Ca2+ fluctuation = 18% and 41% above control, respectively, with or without 10 µM GSK205 pretreatment) or Hypo-osmotic stress (280 mOsm; cell population with intracellular Ca2+ fluctuation = 2% and 83% above iso-osmotic control, respectively, with or without 10 µM GSK205 pretreatment) in primary porcine articular chondrocytes. Also reported to effectively block Ca2+ mobilization induced by 100 nM TRPV4 agonist GSK101 (by 100% with 10 µM GSK205) in murine 3T3-F442A adipocytes in vitro and improve glucose tolerance (1 g/kg glucose via i.p.) in high fat diet-induced obese mice ([peak plasma glucose] = 283 mg/dL vs. 346 mg/dL with or without 7 d 10 mg GSK205/kg/12 h i.p. treatment) in vivo.
FormOrange powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₄H₂₄N₄S • HBr
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (100 mg/ml) or H₂O (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesYe, L., et al. 2012. Cell 151, 96.
Phan, M.N., et al. 2009. Arthritis Rheum. 60, 3028.