生物活性

Rimonabant is the first selective and orally active antagonist of the central brain cannabinoid receptor (CB1) with IC50 with 13.6 nM and EC50 with 17.3 nM in hCB1 transfected HEK 293 membrane .Rimonabant has been used to afford weight reduction and improvements in cardiometabolic risk factors, however is withdrawn in 2009 due to the severe depressive disorder and anxiety.Besides CB1 inhibition ability, Rimonabant is a dual inhibitor of acyl CoA:cholesterol acyltransferases 1 and 2 . Moreover, Rimonabant significantly reduces cell growth and induces cell death of human colorectal cancer cells (DLD-1, CaCo-2 and SW620). Rimonabant is able to alter cell cycle distribution in all the cell lines tested. In the mouse model of azoxymethane-induced colon carcinogenesis, Rimonabant significantly decreased aberrant crypt foci (ACF) formation, which precedes colorectal cancer . Meanwhile, Rimonabant inhibits platelet activation and reduces pro-inflammatory chemokines and leukocytes in Zucker rats .

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。