(S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇
AMG-3969(AMG-3969)
CAS: 1361224-53-4
化学式: C21H20F6N4O3S
| 中文名 | AMG-3969 |
| 英文名 | AMG-3969 |
| 别名 | 化合物AMG-3969 AMG-3969游离态 4-[(2S)-4-[(6-氨基-3-吡啶基)磺酰基]-2-(1-丙炔-1-基)-1-哌嗪基]-Α,Α-双(三氟甲基)-苯甲醇 (S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 |
| 英文别名 | CS-2503 AMG3969 AMG-3969 AMG 3969 Benzenemethanol, 4-[(2S)-4-[(6-amino-3-pyridinyl)sulfonyl]-2-(1-propyn-1-yl)-1-piperazinyl]-α,α-bis(trifluoromethyl)- (S)-2-(4-(4-((6-Aminopyridin-3-yl)sulfonyl)-2-(prop-1-yn-1-yl)piperazin-1-yl)phenyl)-1,1,1,3,3,3-hexafluoropropan-2-ol |
| CAS | 1361224-53-4 |
| 化学式 | C21H20F6N4O3S |
| 分子量 | 522.46 |
| 密度 | 1.56±0.1 g/cm3(Predicted) |
| 沸点 | 648.8±65.0 °C(Predicted) |
| 溶解度 | 溶于DMSO |
| 酸度系数 | 10.12±0.15(Predicted) |
| 存储条件 | 2-8°C(protect from light) |
| 体外研究 | AMG-3969 exhibits potent cellular activity with an EC 50 of 0.202 μM and IC 50 of 4 nM, . It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes). |
| 体内研究 | AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/ob and db/db mice; however,AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose. |
| 参考资料 展开查看 | 1: Bourbeau MP, Ashton KS, Yan J, St Jean DJ Jr. Nonracemic synthesis of GK-GKRP disruptor AMG-3969. J Org Chem. 2014 Apr 18;79(8):3684-7. doi: 10.1021/jo500336e. Epub 2014 Apr 10. PubMed PMID: 24678849. 2: Nishimura N, Norman MH, Liu L, Yang KC, Ashton KS, Bartberger MD, Chmait S, Chen J, Cupples R, Fotsch C, Helmering J, Jordan SR, Kunz RK, Pennington LD, Poon SF, Siegmund A, Sivits G, Lloyd DJ, Hale C, St Jean DJ Jr. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem. 2014 Apr 10;57(7):3094-116. doi: 10.1021/jm5000497. Epub 2014 Mar 31. PubMed PMID: 24611879. 3: St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. PubMed PMID: 24405213. 4: Lloyd DJ, St Jean DJ Jr, Kurzeja RJ, Wahl RC, Michelsen K, Cupples R, Chen M, Wu J, Sivits G, Helmering J, Komorowski R, Ashton KS, Pennington LD, Fotsch C, Vazir M, Chen K, Chmait S, |
(S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.914 ml | 9.57 ml | 19.14 ml |
| 5 mM | 0.383 ml | 1.914 ml | 3.828 ml |
| 10 mM | 0.191 ml | 0.957 ml | 1.914 ml |
| 5 mM | 0.038 ml | 0.191 ml | 0.383 ml |
最后更新：2024-01-02 23:10:35
(S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 - 动物实验
Diabetic db/db mice are used in the study. At 8:00 AM, mice are bled via retro-orbital sinus puncture and blood glucose values are determined and used to randomize the animals in which their averages are similar, and only mice with blood glucose ranges between 300 and 500 mg/dL are included. Vehicle (2% hydroxypropyl methylcellulose, 1% Tween 80, pH 2.2 adjusted with MSA) or AMG-3969 (10, 30, 100 mg/kg) are gavaged at 9:00 AM. Blood glucose is measured at 4, 6, or 8 h posttreatment. At each time point, a 15 μL sample of whole blood is analyzed for drug exposure .
最后更新：2023-08-16 21:32:38
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产品名: (S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 去供应商网站查看 询盘CAS: 1361224-53-4
产地: 北京
包装: 瓶
规格: YS106512-1mg,YS106512-5mg
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库存: 一周左右
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产品名: AMG-3969游离态 去供应商网站查看 询盘CAS: 1361224-53-4
产地: 中国上海
包装: 5mg
规格: 99%
价格: 712.00
库存: 10个工作日
电话: 400-900-4166
手机: 18017137653
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QQ: 3007523013
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产品描述: 中文名：AMG-3969游离态 英文名:AMG-3969 CAS:1361224-53-4 规格:99% 产地:中国上海
提供多种规格现货供应
产品名: (S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇 去供应商网站查看 询盘CAS: 1361224-53-4
产地: 北京
包装: 瓶
规格: YS106512-1mg,YS106512-5mg
价格: 电话、微信、QQ、邮件
库存: 一周左右
电话: 010-50973130
手机: 17801761073(微信同号)
电子邮件: 3193328036@qq.com
QQ: 3193328036
微信: 17801761073
产品描述: 索莱宝直销，欢迎来询
现货供应
产品名: AMG-3969游离态 去供应商网站查看 询盘CAS: 1361224-53-4
产地: 中国上海
包装: 5mg
规格: 99%
价格: 712.00
库存: 10个工作日
电话: 400-900-4166
手机: 18017137653
电子邮件: 3007523013@qq.com
QQ: 3007523013
微信: 18017137653
产品描述: 中文名：AMG-3969游离态 英文名:AMG-3969 CAS:1361224-53-4 规格:99% 产地:中国上海
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