Aurantiamide acetate 是抑制口服有活性的CAThepsin选择性抑制剂,分离自Portulaca oleracea L。它具有抗炎作用,可用于研究炎性相关疾病。
产品描述
Aurantiamide acetate was isolated from the fermentation broth of Aspergillus penicilloides for the first time. Aurantiamide acetate is a selective and orally active cathepsin inhibitor. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2].
体外活性
Aurantiamide acetate decreases viability of U87 and U251 cancer cells in vitro when used at concentrations ranging from 10 to 100 μM. Aurantiamide acetate inhibited cysteine proteinases, in particular, cathepsin L and B with IC50 of 12 microM and 49 microM, respectively.
体内活性
Aurantiamide acetate reduces tumor growth when administered at a dose of 1 mg via intratumoral injection in a U87 mouse xenograft model. In the adjuvant-arthritic rat model, subcutaneously administered 10 mg/kg body weight of this compound suppressed hind paw swelling.
Cas No.
56121-42-7
分子式
C27H28N2O4
分子量
444.52
别名
Asperglaucide;金色酰胺醇酯
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years