Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DS-6930 是一种有效的和选择性的 PPARγ激动剂(EC50= 41 nM)。DS-6930 可有效降低血浆葡萄糖 (PG)水平,此外,与 Rosiglitazone 相比,具有更少的 PPARγ 相关不良反应。DS-6930 在糖尿病中具有研究价值。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 8-10周 | ||
50 mg | ¥ 13,800 | 8-10周 | ||
100 mg | ¥ 17,500 | 8-10周 |
产品描述 | DS-6930 is an potent and selective PPAR γ Agonists with EC50 of 41 nM. DS-6930 can effectively reduce plasma glucose (PG) level, and has less PPARγ-related adverse effects compared with Rosiglitazone. DS-6930 has research value in diabetes. |
体外活性 | DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC 50 =41 nM, E max =68%), and possesses high PPARα or PPARδ selectivity (13% PPARα activation at 10 μM and no PPARδ activation at 10 μM) [1]. DS-6930 (10-100 μM) exhibits lower cell toxicity at 100 μM [1]. |
体内活性 | DS-6930 (0.1-3 mg/kg; p.o. for 3 weeks) decreases plasma glucose (PG) levels in a dose-dependent manner in rats [1]. DS-6930 (100-1000 mg/kg; p.o.for 4 weeks) does not affect any liver enzyme activities and has no remarkable change in relative heart weigh in F344 rats [1]. DS-6930 exhibits C max =0.0792 μg/mL, T max =1.8 h, and AUC 0-24h =0.861 h μg/mL following oral (0.3 mg/kg) administration on day 22 in rats [1]. DS-6930 exhibits C max =2.25 μg/mL, T max =5.0 h, T 1/2 =13.5 h, and AUC last =23.5 h μg/mL following oral (3 mg/kg) administration in cynomolgus monkeys [1]. DS-6930 exhibits excellent bioavailability (F=89%), total body clearance (CL=2.06 mL/min/kg), and distribution volume at steady state (Vss=0.36 L/kg) following intravenous (1 mg/kg) administration in cynomolgus monkeys [1]. Animal Model: Male ZDF rats [1] Dosage: 0.1, 0.3, 1, 3 mg/kg Administration: P.o. daily for 3 weeks Result: 47% PG reduction at dose of 0.3 mg/kg vs vehicle control. Animal Model: Male ZDF rats [1] Dosage: 0.3 mg/kg (Pharmacokinetic Analysis) Administration: P.o. daily for 22 days Result: C max =0.0792 μg/mL; T max =1.8 h; AUC 0-24h =0.861 h μg/mL. |
分子量 | 403.43 |
分子式 | C23H21N3O4 |
CAS No. | 1242328-82-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
DS-6930 1242328-82-0 Inhibitor inhibitor inhibit