| Bioactivity | URB447 is a peripherally restricted CB1 cannabinoid antagonist (IC50: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB1-dependent responses. URB447 can be used for research of obesity[1]. |
| Invitro | URB447 (100 nM-30 μM) 抑制 CB 激动剂 WIN55,212-2 (1 μM) 在大鼠小脑膜制剂诱导的 GTPγS 结合，EC50 为 4.9 μM[1 ]。URB447 (1 μM) 抑制稳定表达小鼠 CB2 受体的 Hek-293 细胞中 β-肾上腺素能激动剂异丙肾上腺素 (10 μM) 诱导的 cAMP 积累[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> URB447 相关抗体: |
| In Vivo | URB447 (20 mg/kg，腹腔注射) 可减少瑞士小鼠的总食物消耗，并显示 Cmax 为 596 nM[1]。URB447 (20 mg/kg，腹腔注射) 可阻断瑞士小鼠中 Methanandamide 的镇痛作用，表明 URB447 抑制外周 CB1 介导的镇痛[1]。URB447 (20 mg/kg，腹腔注射，每天一次，持续 2 周) 可减少肥胖 ob/ob 小鼠的食物消耗和体重增加[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 1132922-57-6 |
| Formula | C25H21ClN2O |
| Molar Mass | 400.90 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. LoVerme J, et al. Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice. Bioorg Med Chem Lett. 2009 Feb 1;19(3):639-43. |