store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Saxagliptin (BMS-477118) 是一种选择性,可逆性,竞争性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin 能够用于 2 型糖尿病的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 622 | 现货 | ||
25 mg | ¥ 1,160 | 现货 | ||
50 mg | ¥ 1,830 | 现货 | ||
100 mg | ¥ 2,820 | 现货 | ||
200 mg | ¥ 3,970 | 现货 | ||
500 mg | ¥ 6,450 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 435 | 现货 |
产品描述 | Saxagliptin (BMS-477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM. |
靶点活性 | DPP-4:26 nM |
体外活性 | 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). [2] Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion. [3] |
体内活性 | 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. [4] |
别名 | BMS-477118, 沙克列汀, Onglyza, 沙格列汀 |
分子量 | 315.41 |
分子式 | C18H25N3O2 |
CAS No. | 361442-04-8 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 59 mg/mL (187.1 mM)
H2O: 58 mg/mL (183.9 mM)
Ethanol: 23 mg/mL (72.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / H2O / Ethanol | 1 mM | 3.1705 mL | 15.8524 mL | 31.7048 mL | 79.2619 mL |
5 mM | 0.6341 mL | 3.1705 mL | 6.341 mL | 15.8524 mL | |
10 mM | 0.317 mL | 1.5852 mL | 3.1705 mL | 7.9262 mL | |
20 mM | 0.1585 mL | 0.7926 mL | 1.5852 mL | 3.9631 mL | |
50 mM | 0.0634 mL | 0.317 mL | 0.6341 mL | 1.5852 mL | |
DMSO / H2O | 100 mM | 0.0317 mL | 0.1585 mL | 0.317 mL | 0.7926 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Saxagliptin 361442-04-8 Proteases/Proteasome Ubiquitination Proteasome DPP-4 BMS-477118 Inhibitor p-AKT DPP β-catenin Dipeptidyl Peptidase inhibit insulin 沙克列汀 Onglyza c-myc 沙格列汀 proliferation glucagon peptide-1 BMS477118 diabetes glucagon-like BMS 477118 inhibitor