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沙格列汀 /Saxagliptin {[allProObj[0].p_purity_real_show]}

货号：A354223 同义名： 沙克列汀 / BMS-477118

Saxagliptin is a selective and reversible DPP4 inhibitor with IC50 of 26 nM.

Saxagliptin 化学结构 CAS号：361442-04-8
Saxagliptin 化学结构
CAS号：361442-04-8
Saxagliptin 3D分子结构
CAS号：361442-04-8
Saxagliptin 化学结构 CAS号：361442-04-8
Saxagliptin 3D分子结构 CAS号：361442-04-8
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Saxagliptin 纯度/质量文件 产品仅供科研

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Saxagliptin 生物活性

描述 Saxagliptin is a dipeptidyl peptidase 4 (DPP-4) inhibitor. DPP-4 inhibition with saxagliptin did not increase or decrease the rate of ischemic events, though the rate of hospitalization for heart failure was increased[3]. Generally, saxagliptin has similar efficacy compared with most oral antidiabetic drugs and may be more effective than acarbose, while having a better safety profile than both acarbose and sulfonylureas[4]. Saxagliptin has a shorter half-life than the other dipeptidyl-peptidase IV inhibitors, so it might be a better choice among drugs in this class for nursing mothers[5]. Dipeptidyl peptidase 4 inhibitors may have a protective effect in diabetic nephropathy. Treatment with saxagliptin improved ACR, even in the normoalbuminuric range, without affecting EGFR[6].

Saxagliptin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
Caco-2 cells Function assay Inhibition of human DPP4 expressed in Caco-2 cells, Ki=0.6 nM 17034148

Saxagliptin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01646320 - Completed - -
NCT02377388 Platelet Aggregation During Ac... 展开 >>ute Myocardial Infarction 收起 << Phase 3 Recruiting December 2019 Brazil ... 展开 >> Heart Institute(InCor)-Acute Coronary Care Unit Recruiting São Paulo, SP, Brazil, 01406000 Contact: Paulo R Genestreti, MD    55 11 2661-5058    paulo.gen@ig.com.br    Principal Investigator: Jose C Nicolau, MD,PhD          Sub-Investigator: Paulo R Genestreti, MD 收起 <<
NCT01646320 Type 2 Diabetes Phase 3 Completed - -

Saxagliptin 参考文献

[1]Leiter LA, Teoh H, Braunwald E, et al. Efficacy and safety of saxagliptin in older participants in the SAVOR-TIMI 53 trial. Diabetes Care. 2015 Jun;38(6):1145-53.

[2]Tahrani AA, Piya MK, et al. Saxagliptin: a new DPP-4 inhibitor for the treatment of type 2 diabetes mellitus. Adv Ther. 2009 Mar;26(3):249-62.

[3]Scirica BM, Bhatt DL, Braunwald E, Steg PG, Davidson J, Hirshberg B, Ohman P, Frederich R, Wiviott SD, Hoffman EB, Cavender MA, Udell JA, Desai NR, Mosenzon O, McGuire DK, Ray KK, Leiter LA, Raz I; SAVOR-TIMI 53 Steering Committee and Investigators. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus. N Engl J Med. 2013 Oct 3;369(14):1317-26

[4]Men P, Li XT, Tang HL, Zhai SD. Efficacy and safety of saxagliptin in patients with type 2 diabetes: A systematic review and meta-analysis. PLoS One. 2018 May 22;13(5):e0197321

[5]Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Saxagliptin. 2019 Feb 7

[6]Mosenzon O, Leibowitz G, Bhatt DL, Cahn A, Hirshberg B, Wei C, Im K, Rozenberg A, Yanuv I, Stahre C, Ray KK, Iqbal N, Braunwald E, Scirica BM, Raz I. Effect of Saxagliptin on Renal Outcomes in the SAVOR-TIMI 53 Trial. Diabetes Care. 2017 Jan;40(1):69-76

Saxagliptin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.85mL

3.17mL

1.59mL

31.70mL

6.34mL

3.17mL

Saxagliptin 技术信息

CAS号361442-04-8
分子式C18H25N3O2
分子量 315.41
别名 沙克列汀 ;BMS-477118
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 35 mg/mL(110.97 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(31.7 mM)，配合低频超声助溶
动物实验配方

Tags: Saxagliptin | BMS-477118 | 沙克列汀 | Diabete | DPP4 | AmBeed-信号通路专用抑制剂 | Saxagliptin 纯度/质量文件 | Saxagliptin 生物活性 | Saxagliptin 细胞研究 | Saxagliptin 临床数据 | Saxagliptin 参考文献 | Saxagliptin 实验方案 | Saxagliptin 技术信息

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