Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ki16198 是一种可口服的 LPA 受体拮抗剂,是 Ki16425 的甲酯衍生物。它抑制 LPA1 和 LPA3 诱导的肌醇磷酸的Ki 值分别为 0.34 和 0.93 μM,可用于胰腺癌发生和转移的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 328 | 现货 | ||
5 mg | ¥ 823 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,890 | 现货 | ||
50 mg | ¥ 4,370 | 现货 | ||
100 mg | ¥ 6,230 | 现货 | ||
500 mg | ¥ 12,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 913 | 现货 |
产品描述 | Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6. |
靶点活性 | LPA3:0.93 μM(Ki), LPA1:0.34 μM(Ki) |
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] |
分子量 | 488.98 |
分子式 | C24H25ClN2O5S |
CAS No. | 355025-13-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 89 mg/mL (182 mM)
Ethanol: 33 mg/mL (67.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.0451 mL | 10.2254 mL | 20.4507 mL | 51.1268 mL |
5 mM | 0.409 mL | 2.0451 mL | 4.0901 mL | 10.2254 mL | |
10 mM | 0.2045 mL | 1.0225 mL | 2.0451 mL | 5.1127 mL | |
20 mM | 0.1023 mL | 0.5113 mL | 1.0225 mL | 2.5563 mL | |
50 mM | 0.0409 mL | 0.2045 mL | 0.409 mL | 1.0225 mL | |
DMSO | 100 mM | 0.0205 mL | 0.1023 mL | 0.2045 mL | 0.5113 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。
Ki16198 355025-13-7 GPCR/G Protein LPA Receptor LPL Receptor lung Ki 16198 inhibit Inhibitor BxPC-3 liver metastasis Ki-16198 Lysophospholipid Receptor inhibitor