| Bioactivity | CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model[1]. |
| Invitro | CB1 inverse agonist 2 (compound 12 h) 对 CB1 具有选择性,对 CB1 和 CB2 的 pKi 值分别为 9.7 和 6.0[1]。 |
| In Vivo | CB1 inverse agonist 2 (compound 12 h) (1 mg/kg; 腹腔注射; 单次剂量) 对体温降低的抑制程度达到 70%,(10mg /kg;口服; 单剂量) 对食物摄入的抑制率达到 59%[1]。CB1 inverse agonist 2 (10 mg/kg; 口服; 每天一次,持续 14 天) 导致小鼠体重与初始体重相比,出现 13% 的减轻[1]。 |
| Name | CB1 inverse agonist 2 |
| CAS | 1019839-52-1 |
| Formula | C24H20ClFN2OS |
| Molar Mass | 438.94 |
| 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]. Synthesis and Evaluation of Dibenzothiazepines: A Novel Class of Selective Cannabinoid-1 Receptor Inverse AgonistsJ. Med. Chem., 2009, 52 (7), pp 1975-1982 [2]. Pettersson H, et al. Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. J Med Chem. 2009 Apr 9;52(7):1975-82. |