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- 2025年12月18日
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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：
Saxagliptin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
361442-04-8
- 规格：
100mg/10mg/1mg/50mg/25mg/5mg
| 规格： | 100mg | 产品价格： | ￥1810.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥480.0 |
| 规格： | 1mg | 产品价格： | ￥166.0 |
| 规格： | 50mg | 产品价格： | ￥1216.0 |
| 规格： | 25mg | 产品价格： | ￥796.0 |
| 规格： | 5mg | 产品价格： | ￥340.0 |
Saxagliptin是选择性可逆的DPP4抑制剂。
| 基本信息 | |
| CAS | No.361442-04-8 |
| 中文名称 | 沙格列汀 |
| 英文名称 | Saxagliptin |
| 别名 | BMS-477118;沙克列汀;Onglyza |
| 分子式 | C18H25N3O2 |
| 分子量 | 315.41 |
| 溶解性 | Soluble in Water/DMSO ≥1mg/mL |
| 纯度 | ≥99% |
| 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 |
| EC | EINECS 1308068-626-2 |
| MDL | MFCD12756398 |
| SMILES | N#C[C@@H]1C[C@]2([H])[C@](C2)([H])N1C([C@H]([C@@]34C[C@@H]5C[C@H](C4)C[C@](C5)(O)C3)N)=O |
| 靶点 | Dipeptidyl Peptidase (DPP) |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | Saxagliptin是选择性可逆的DPP4抑制剂。 |
| 生物活性 | Saxagliptin (BMS-477118) is a potent， selective， reversible， competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research[1][2][3]. |
| In Vitro | Saxagliptin (100?nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation[1].Saxagliptin (100?nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels， paralleled with the increase of c-myc and cyclin D1 protein expression[1].Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon[3].Cell Viability Assay[1]：Cell Line:INS-1 832/13 cells；Concentration:100?nM；Incubation Time:48 hours；Result:Significantly induced β-cell proliferation.Western Blot Analysis[1]：Cell Line:INS-1 832/13 cells；Concentration:100?nM；Incubation Time:48 hours；Result:Increased the p-AKT and active β-catenin protein levels， paralleled with the increase of c-myc and cyclin D1 protein expression. |
| 细胞实验 | Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats， significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed[1].Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats， by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose， ~20% and 70% inhibition， respectively， remained[2]. |
| 数据来源文献 | [1]. Chun-Jun Li， et al. Saxagliptin Induces β-Cell Proliferation through Increasing Stromal Cell-Derived Factor-1α In Vivo and In Vitro. Front Endocrinol (Lausanne). 2017 Nov 27;8:326. [2]. Darshan J Dave. Saxagliptin: A dipeptidyl peptidase-4 inhibitor in the treatment of type 2 diabetes mellitus. J Pharmacol Pharmacother. 2011 Oct;2(4):230-5. [3]. Carolyn F Deacon， et al. Saxagliptin: a new dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes. Adv Ther. 2009 May;26(5):488-99. |
| 单位 | 瓶 |
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IS1520 沙格列汀 代谢酶/蛋白酶 索莱宝
￥166 - 1810
