≥99% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at 2-8°C,Desiccated Ships Wet ice Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
GSK205 is a potent, selective TRPV4 antagonist with an IC 50 of 4.19 μM for inhibiting TRPV4 -mediated Ca 2+ influx
In Vitro
GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist. ?\nGSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: T3-F442A adipocytes Concentration: 5 μM Incubation Time: 4 days Result: Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.
In Vivo
GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss . ?\nGSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J mice with high-fat diet Dosage: 10 mg/kg Administration: Intraperitoneal injection; twice daily; for 7 days Result: Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.
Form:Solid
IC50& Target:IC50: 4.19 μM (TRPV4)
| Canonical Smiles | CN(CCC1=CC=C(C=C1)NC2=NC=C(S2)C3=CN=CC=C3)CC4=CC=CC=C4.Br |
|---|---|
| IUPAC Name | N-[4-[2-[benzyl(methyl)amino]ethyl]phenyl]-5-pyridin-3-yl-1,3-thiazol-2-amine;hydrobromide |
| InChIKey | LQGOJHGNGSOUKL-UHFFFAOYSA-N |
| INCHI | 1S/C24H24N4S.BrH/c1-28(18-20-6-3-2-4-7-20)15-13-19-9-11-22(12-10-19)27-24-26-17-23(29-24)21-8-5-14-25-16-21;/h2-12,14,16-17H,13,15,18H2,1H3,(H,26,27);1H |
| Isomeric SMILES | CN(CCC1=CC=C(C=C1)NC2=NC=C(S2)C3=CN=CC=C3)CC4=CC=CC=C4.Br |
| PubChem CID | 72736243 |
| Molecular Weight | 481.5 |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Class | Benzene and substituted derivatives |
| Subclass | Phenethylamines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Phenethylamines |
| Alternative Parents | Phenylmethylamines Benzylamines Aniline and substituted anilines Aralkylamines 2,5-disubstituted thiazoles Pyridines and derivatives 2-amino-1,3-thiazoles Heteroaromatic compounds Trialkylamines Azacyclic compounds Hydrocarbon derivatives Hydrobromides |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Phenethylamine - Benzylamine - Phenylmethylamine - Aniline or substituted anilines - 2,5-disubstituted 1,3-thiazole - Aralkylamine - 1,3-thiazol-2-amine - Pyridine - Azole - Heteroaromatic compound - Thiazole - Tertiary amine - Tertiary aliphatic amine - Azacycle - Organoheterocyclic compound - Hydrobromide - Amine - Organonitrogen compound - Hydrocarbon derivative - Organic nitrogen compound - Aromatic heteromonocyclic compound |
| Description | This compound belongs to the class of organic compounds known as phenethylamines. These are compounds containing a phenethylamine moiety, which consists of a phenyl group substituted at the second position by an ethan-1-amine. |
| External Descriptors | Not available |
| Solubility | DMSO : 250 mg/mL (519.26 mM; Need ultrasonic) |
|---|---|
| Molecular Weight | 481.500 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 2 |
| Hydrogen Bond Acceptor Count | 5 |
| Rotatable Bond Count | 8 |
| Exact Mass | 480.098 Da |
| Monoisotopic Mass | 480.098 Da |
| Topological Polar Surface Area | 69.300 Ų |
| Heavy Atom Count | 30 |
| Formal Charge | 0 |
| Complexity | 462.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
