| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| S408204-1ml |
1ml |
现货  |
|
| 别名 | 沙格列汀(BMS-477118) |
|---|---|
| 英文别名 | Onglyza | 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-, (1S,3S,5S)- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Saxagliptin (BMS-477118) |
| 生化机理 | 沙克列汀（BMS-477118，Onglyza）是一种选择性和可逆性 DPP4 抑制剂，IC50 为 26 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 二肽基肽酶 4 抑制剂 |
| 产品介绍 |
Saxagliptin(BMS477118)是选择性可逆的DPP4抑制剂，IC50和Ki分别为26 nM和1.3 nM。 Information Saxagliptin (BMS-477118) Saxagliptin (BMS-477118, Onglyza) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9). Saxagliptin reduces the degradation of the incretin hormone Glukagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of Glukagon secretion. In vivo Maximal responses of Saxagliptin in glucose excursion in Zuckerfa/fa rats are associated with plasma DPP4 inhibition of approximately 60% vs. control, and no additional antihyperglycemic effects are seen at higher percent inhibition. Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT. cell lines：MZ-CRC-1 and TT cells Concentrations： Incubation Time： Powder Purity:≥96% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | NC(C(=O)N1C(CC2CC12)C#N)[C]34CC5[CH2]C(C[C](O)(C5)C3)C4 |
| 分子量 | 315.41 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (123.18 mM); Water: 100 mg/mL (123.18 mM); Ethanol: 100 mg/mL (123.18 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| NMR Spectrum 1H | Conforms to Structure |
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