GSK205 HBr
- CAS No.
- 1263068-83-2
- Chemical Name:
- GSK205 HBr
- Synonyms
- GSK205;GSK205 HBr;N-(4-(2-(Benzyl(methyl)amino)ethyl)phenyl)-5-(pyridin-3-yl)thiazol-2-amine hydrobromide
- CBNumber:
- CB25494080
- Molecular Formula:
- C24H25BrN4S
- Molecular Weight:
- 481.46
- MDL Number:
- MOL File:
- 1263068-83-2.mol
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P264-P270-P301+P312-P330-P501 |
GSK205 HBr price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0103037 | GSK205 99.45% | 1263068-83-2 | 5mg | $190 | 2021-12-16 | Buy |
| ChemScene | CS-0103037 | GSK205 99.45% | 1263068-83-2 | 10mg | $330 | 2021-12-16 | Buy |
| ChemScene | CS-0103037 | GSK205 99.45% | 1263068-83-2 | 25mg | $710 | 2021-12-16 | Buy |
| ChemScene | CS-0103037 | GSK205 99.45% | 1263068-83-2 | 50mg | $1200 | 2021-12-16 | Buy |
| ChemScene | CS-0103037 | GSK205 99.45% | 1263068-83-2 | 100mg | $2100 | 2021-12-16 | Buy |
GSK205 HBr Chemical Properties,Uses,Production
Uses
GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19? μM for inhibiting TRPV4-mediated Ca2+ influx[1][2].
Biological Activity
GSK205 is a potent and selective TRPV4 antagonist with IC50 of 4.19 μM, inhibits TRPV4-mediated Ca2+ influx.
in vitro
GSK205 HBr (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist.
GSK205 (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. < /p>
RT-PCR
| Cell 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 decre ase in the proinflammatory gene program. |
in vivo
GSK205 HBr (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 . It 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.
It has a relatively short half-life of 2 hours in the plasma and adipose tissues.
| Animal Model: | Male C57BL/ 6J mice with high-fat diet |
| Dosage: | 10 mg/kg | < /tr>
| Administration: | Intraperitoneal injection; twice daily; for 7 days < /td> |
| 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. |
References
[1] Ye L, et al. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012 Sep 28;151(1):96-110. DOI:10.1016/j.cell.2012.08.034
[2] Kanju P, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci Rep. 2016 Jun 1;6:26894. DOI:10.1038/srep26894
GSK205 HBr Preparation Products And Raw materials
Raw materials
Preparation Products
GSK205 HBr Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 32286 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Shanghai Raise Chemical Technology Co.,Ltd | 15026594951 | rs@raise-chem.com | China | 4075 | 55 |
| Nanjing XiZe Biotechnology CO., Ltd. | 025-66023220 0086-15250997978 | 1511893459@qq.com | China | 8391 | 55 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9729 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
| Shanghai hongqu biomedical technology co. LTD | 88888888888 | hongquchem@qq.com | China | 5132 | 58 |
| ShangHai ChuanQian Chemcial Technique Centre | 15869524721 | 3525679403@qq.com | China | 4592 | 58 |