Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TM38837 是外周选择性大麻素受体1型受体拮抗剂。它减少精神病副作用的倾向。它对大脑的渗透率有限,以降低或防止 CNS 不良反应,并保留潜在的抗肥胖作用。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 511 | 现货 | ||
5 mg | ¥ 1,220 | 现货 | ||
10 mg | ¥ 1,620 | 现货 | ||
25 mg | ¥ 2,730 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,820 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,550 | 现货 |
产品描述 | TM38837 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes. |
体内活性 | TM38837, a novel, largely peripherally restricted CB1 antagonist, in terms of fear-promoting consequences of systemic vs. intracerebral injections.?Different groups of male C57BL/6 N mice underwent auditory fear conditioning, followed by re-exposure to the tone.?Mice were treated per os (p.o.) with TM38837 (10, 30, or 100 mg/kg), rimonabant (10 mg/kg;?a brain penetrating CB1 antagonist/inverse agonist which served as a positive control), or vehicle, 2 h prior the tone presentation.?Only the high dose of TM38837 (100 mg/kg) induced a significant increase in freezing behavior, similar to that induced by rimonabant (10 mg/kg) (p 0.001).?If injected into the brain both TM38837 (10 or 30 μg/mouse) and rimonabant (1 or 10 μg/mouse) caused a sustained fear response to the tone, which was more pronounced after rimonabant treatment.?Taken together, TM38837 was at least one order of magnitude less effective in promoting fear responses than rimonabant.?Given the equipotency of the two CB1 antagonists with regard to weight loss and metabolic syndrome-like symptoms in rodent obesity models, our results point to a critical dose range in which TM3887 might be beneficial for indications such as obesity and metabolic disorders with limited risk of fear-promoting effects[1]. |
分子量 | 617.51 |
分子式 | C30H25Cl2F3N4OS |
CAS No. | 1253641-65-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 40 mg/mL (64.77 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6194 mL | 8.097 mL | 16.1941 mL | 40.4852 mL |
5 mM | 0.3239 mL | 1.6194 mL | 3.2388 mL | 8.097 mL | |
10 mM | 0.1619 mL | 0.8097 mL | 1.6194 mL | 4.0485 mL | |
20 mM | 0.081 mL | 0.4049 mL | 0.8097 mL | 2.0243 mL | |
50 mM | 0.0324 mL | 0.1619 mL | 0.3239 mL | 0.8097 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。
TM38837 1253641-65-4 GPCR/G Protein Cannabinoid Receptor peripheral CB1 TM-38837 antiobesity TM 38837 inhibit fat Inhibitor metabolic fear inhibitor