扁塑藤素
中文名称 | 扁塑藤素 |
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中文同义词 | 扁塑藤素 (扁蒴藤素);扁蒴藤素;扁塑藤素;扁塑藤素 标准品;单酰基甘油脂肪酶(MGL)抑制剂(PRISTIMERIN);扁塑藤素对照品;标准品对照品】PRISTIMERIN;(2R,4AS,6AS,12BR,14AS,14BR)-10-羟基-2,4A,6A,9,12B,14A-六甲基-11-氧代-1,2,3,4,4A,5,6,6A,11,12B,13,14,14A,14B-十四氢苉-2-羧酸甲酯 |
英文名称 | pristimerin |
英文同义词 | pristimerin;3-Hydroxy-2-oxo-24-nor-D:A-friedoolean-1(10),3,5,7-tetren-29-oic acid methyl ester;Celastrol-methylether;(9β,13α,14β,20α)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oicacidmethylester;(9b,13a,14b,20a)-3-Hydroxy-9,13-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tertraen-29-oic acid methyl ester;3-hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid, methyl ester;Celastrol methyl ester;Pristimerin(NSC 99281) |
CAS号 | 1258-84-0 |
分子式 | C30H40O4 |
分子量 | 464.64 |
EINECS号 | 251-228-4 |
相关类别 | 对照品,标准品;植物提取物;对照品;标准品;中药对照品;科研试剂;标准品-对照品;细胞生物学试剂;分析试剂标准品;对照品-中药对照品;标准品 -中药标准品;标准品,对照品;医药、农药及染料中间体;蒽醌 |
Mol文件 | 1258-84-0.mol |
结构式 |
扁塑藤素 性质
熔点 | 219.5°C |
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沸点 | 488.1°C (rough estimate) |
密度 | 1.0271 (rough estimate) |
折射率 | 1.4800 (estimate) |
储存条件 | -20°C |
溶解度 | 二甲基亚砜:≥5mg/mL |
形态 | 红色固体 |
酸度系数(pKa) | 8.60±0.70(Predicted) |
颜色 | 橙色 |
IC50: 93 nM (MGL)
Pristimerin inhibits the activity of purified MGL with an IC 50 of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC 50 of 398±68 nM. Pristimerin inhibits MGL through a mechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might be strengthened by formation of a polar interaction with a regulatory cysteine, possibly Cys 208 . Pristimerin inhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreases VEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-induced VEGFR2-mediated signaling pathway .
Pristimerin inhibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density in synovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera, including TNF-α, Ang-1, and MMP-9.
安全信息
毒性 | LD50 oral in mouse: 8gm/kg |
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更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-N1937 | Pristimerin | 1 mg | 316元 | |
2024/08/19 | HY-N1937 | 扁塑藤素 Pristimerin | 1258-84-0 | 5mg | 748元 |