| 中文名称: | GSK205 | ||||
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| 英文名称: | GSK205 | ||||
| 别名: | GSK205 GSK205 | ||||
| CAS No: | 1263068-83-2 | 分子式: | C24H25BrN4S | 分子量: | 481.45 |
| CAS No: | 1263068-83-2 | ||||
| 分子式: | C24H25BrN4S | ||||
| 分子量: | 481.45 | ||||
基本信息
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产品编号： |
G10591 |
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产品名称： |
GSK205 |
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CAS: |
1263068-83-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
481.45 |
-20℃ |
1个月 |
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化学名： |
N-[4-[2-[benzyl(methyl)amino]ethyl]phenyl]-5-pyridin-3-yl-1,3-thiazol-2-amine;hydrobromide |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.0771mL |
10.3853mL |
20.7706mL |
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5mM |
0.4154mL |
2.0771mL |
4.1541mL |
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10mM |
0.2077mL |
1.0385mL |
2.0771mL |
生物活性
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产品描述 |
一种高效的，选择性的TRPV4拮抗剂 |
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靶点 |
IC50:4.19μM (TRPV4) |
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体外研究 |
GSK205 (100μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes,as it effectively blocks the calcium influx caused by TRPV4 agonist.GSK205 (5μM;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. RT-PCR |
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Cell Line: |
T3-F442A adipocytes |
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Concentration: |
5μM |
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Incubation Time: |
4 days |
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Result: |
Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program. |
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体内研究 |
GSK205 (10mg/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.GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues. |
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Animal Model: |
Male C57BL/6J mice with high-fat diet |
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Dosage: |
10mg/kg |
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Administration: |
Intraperitoneal injection;twice daily;for 7 days |
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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. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
