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- 详细信息
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
BMS-816336
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
1009583-20-3
- 规格:
10mg/1mg/5mg
| 规格: | 10mg | 产品价格: | ¥5490.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥1580.0 |
| 规格: | 5mg | 产品价格: | ¥3490.0 |
| 基本信息 | |
| CAS | No.1009583-20-3 |
| 英文名称 | BMS-816336 |
| 分子式 | C21H27NO3 |
| 分子量 | 341.44 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| SMILES | C1C2CC3CC(C2O)CC1C3(CC(=O)N4CC(C4)O)C5=CC=CC=C5 |
| InChIKey | OAAZMUGLOXGVNH-UHFFFAOYSA-N |
| InChI | InChI=1S/C21H27NO3/c23-18-11-22(12-18)19(24)10-21(15-4-2-1-3-5-15)16-6-13-7-17(21)9-14(8-16)20(13)25/h1-5,13-14,16-18,20,23,25H,6-12H2 |
| PubChem CID | 59336911 |
| 靶点 | 11β-HSD |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | BMS-816336 是一种有效的 11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂。 |
| 生物活性 | BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM[1]. |
| IC50 | IC50: 3.0nM(11β-HSD1)[1] |
| In Vitro | 11β-HSD1 inhibition may be useful in the treatment of type II diabetes and other potential clinical utilities such as atheroprotection and cognitive protection. BMS-816336(6n-2)inhibits 11β-HSD1 enzyme in HEK and 3T3L1 cells with IC50s of 37.3 and 28.6 nM,respectively[1]. |
| 细胞实验 | BMS-816336 represents a potential new treatment for type 2 diabetes,metabolic syndrome,and other human diseases modulated by glucocorticoid control. BMS-816336(6n-2)exhibits a robust acute pharmacodynamic effect in cynomolgus monkeys(ED50=0.12 mg/kg)and in DIO mice(1,3,10,30,100 mg/kg,120 mintues). It is orally bioavailable(%F ranges from 20 to 72% in preclinical species)and has a predicted pharmacokinetic profile of a high peak to trough ratio and short half-life in humans[1]. |
| 数据来源文献 | [1]. Ye XY, et al. Discovery of Clinical Candidate 2-((2S,6S)-2-Phenyl-6-hydroxyadamantan-2-yl)-1-(3'-hydroxyazetidin-1-yl)ethanone [BMS-816336], an Orally Active Novel Selective 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor. J Med Chem. 2017 Jun 22;60(12):4932-4948. |
| 单位 | 瓶 |
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IB3650 BMS-816336 代谢酶/蛋白酶 索莱宝
¥1580 - 5490










