Chemical Name |
Pristimerin |
CAS Number |
1258-84-0 |
MDL Number |
MFCD01711331 |
Molecular Formula |
C30H40O4 |
Molecular Weight |
464.64 |
Synonyms |
Celastrol methyl ester |
Introduction of 1258-84-0 :
Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM. IC50 & Target: IC50: 93 nM (MGL)[1] In Vitro: Pristimerin inhibits the activity of purified MGL with an IC50 of 93±8 nM and that of non-purified MGL (cell lysates of MGL-transfected HeLa cells) with an IC50 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 Cys208[1]. 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 [2]. In Vivo: 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[2].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.