Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KGA-2727是选择性,高亲和力和口服有效的 SGLT1抑制剂,对人和大鼠 SGLT1的 Ki 分别为 97.4 nM 和 43.5 nM,对 SGLT1的选择性比人SGLT2 高 140 倍 ,大鼠SGLT2高390 倍。KGA-2727具有抗糖尿病活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,080 | 现货 | ||
2 mg | ¥ 1,660 | 现货 | ||
5 mg | ¥ 2,770 | 现货 | ||
10 mg | ¥ 4,120 | 现货 | ||
25 mg | ¥ 6,590 | 现货 | ||
50 mg | ¥ 8,970 | 现货 | ||
100 mg | ¥ 12,100 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,420 | 现货 |
产品描述 | KGA-2727 is a potent and selective SGLT1 inhibitor, with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 for the treatment of diabete. |
靶点活性 | hSGLT1:(ki)97.4 nM, rat SGLT1:43.5 nM(ki) |
体外活性 | KGA-2727, which has a pyrazole-O-glucoside structure, as the first selective SGLT1 inhibitor.?KGA-2727 inhibited SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs.KGA2727 dose-dependently inhibits Methyl-Dglucopyranoside (AMG) uptake by SGLT1 and SGLT2.?A Dixon plot analysis for KGA-2727 shows good linearity for human SGLT1 and SGLT2.?KGA-2727 inhibits these SGLTs in a competitive manner displayed from the results of the Dixon plot. |
体内活性 | In a small intestine closed loop absorption test with normal rats, KGA-2727 inhibited the absorption of glucose but not that of fructose.?After oral intake of starch along with KGA-2727 in normal rats, the residual content of glucose in the gastrointestinal tract increased.?In the oral glucose tolerance test with streptozotocin-induced diabetic rats, KGA-2727 attenuated the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improved postprandial hyperglycemia.?In Zucker diabetic fatty (ZDF) rats, chronic treatments with KGA-2727 reduced the levels of plasma glucose and glycated hemoglobin.?Furthermore, KGA-2727 preserved glucose-stimulated insulin secretion and reduced urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.?In addition, the chronic treatment with KGA-2727 increased the level of glucagon-like peptide-1 in the portal vein. |
分子量 | 536.62 |
分子式 | C26H40N4O8 |
CAS No. | 666842-36-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (186.35 mM), sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8635 mL | 9.3176 mL | 18.6352 mL | 46.5879 mL |
5 mM | 0.3727 mL | 1.8635 mL | 3.727 mL | 9.3176 mL | |
10 mM | 0.1864 mL | 0.9318 mL | 1.8635 mL | 4.6588 mL | |
20 mM | 0.0932 mL | 0.4659 mL | 0.9318 mL | 2.3294 mL | |
50 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.9318 mL | |
100 mM | 0.0186 mL | 0.0932 mL | 0.1864 mL | 0.4659 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。
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