Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Olorinab (APD 371) (APD 371) 是大麻素受体 2 型 (CB2) 强有效的、选择性的全激动剂,其对 hCB2 的EC50 值为 6.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 521 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,990 | 现货 | ||
25 mg | ¥ 3,990 | 现货 | ||
50 mg | ¥ 5,680 | 现货 |
产品描述 | Olorinab (APD 371) (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist. With an EC50 of 6.2 nM for hCB2. |
靶点活性 | CB2 (human):(EC50)6.2 nM |
体外活性 | A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed. Olorinab (APD 371) is highly selective for CB2 over CB1 in both binding and functional assays. Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB2 suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling[1]. |
体内活性 | Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED50=2.3 mg/kg). The analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB2 receptors[1]. In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. |
别名 | APD 371 |
分子量 | 357.41 |
分子式 | C18H23N5O3 |
CAS No. | 1268881-20-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 180 mg/mL (503.6 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 | 2.7979 mL | 13.9895 mL | 27.9791 mL | 69.9477 mL |
5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL | 13.9895 mL | |
10 mM | 0.2798 mL | 1.399 mL | 2.7979 mL | 6.9948 mL | |
20 mM | 0.1399 mL | 0.6995 mL | 1.399 mL | 3.4974 mL | |
50 mM | 0.056 mL | 0.2798 mL | 0.5596 mL | 1.399 mL | |
100 mM | 0.028 mL | 0.1399 mL | 0.2798 mL | 0.6995 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。
Olorinab 1268881-20-4 GPCR/G Protein Cannabinoid Receptor APD 371 APD-371 APD371 Inhibitor inhibitor inhibit