Pristimerin-Celastrol-methyl-ester-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPristimerinCat. No.: HY-N1937CAS No.: 1258-84-0Synonyms: Celastrol methyl ester分式: CHO分量: 464.64作靶點: Bacterial作通路: Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 20 mg/mL (43

2、.04 mM; Need ultrasonic)H2O : 90% corn oilSolubility: 2 mg/mL (4.30 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Pristimerin效可逆的單酰 油脂肪酶(MGL)抑制劑，IC50值為93 nM。IC50 & Target IC50: 93 nM (MGL) 1體外研究 Pristimerin inhibits the activity of purified MGL with an IC

3、50 of 938 nM and that of non-purified MGL (celllysates of MGL-transfected HeLa cells) with an IC50 of 39868 nM. Pristimerin inhibits MGL through amechanism that is rapid, reversible and non-competitive. The binding of pristimerin to MGL might bestrengthened by formation of a polar interaction with a

4、 regulatory cysteine, possibly Cys208 1. Pristimerininhibits HFLS-RA and HUVEC cell viability in a dose- and time-dependent manner. Pristimerin decreasesVEGF-induced autophosphorylation of VEGFR2 and attenuates the activation of the VEGF-inducedVEGFR2-mediated signaling pathway 2.體內研究 Pristimerin in

5、hibits inflammation and tumor angiogenesis. Pristimerin significantly reduces vessel density insynovial membrane tissues of inflamed joints and reduces the expression of pro-angiogenic factors in sera,including TNF-, Ang-1, and MMP-9 2.PROTOCOLCell Assay 2 HFLS-RA (5 103 cells/mL) or HUVECs (1 104 c

6、ells/well) are seeded in 96-well plates and cultured innormal growth medium for 24 h. The cells are then incubated with different Pristimerin concentrations (0,0.125, 0.25, 0.5 M). The effects of Pristimerin on HUVECs viability are determined under VEGF-inducedconditions. Cell viability is quantifie

7、d by MTT assay. At 4 h before the end of the culture period, 30 L of MTTsolution (5.0 mg/mL) is added to each well. Cells without Pristimerin or VEGF served as a vehicle control 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rat: Pristimerin i

8、s dissolved in DMSO (0.4%) and intraperitoneally injected daily into Male Sprague-DawleyAdministration rats in the experimental group (low-dose group, 0.40 mg/kg of body weight; high-dose group, 0.80 mg/kg ofbody weight) from day 11 to day 24 of immunization. The model group received vehicle (DMSO,

9、0.4%), andthe normal control group received normal saline (NS). Methotrexate (positive control) is suspended in NS andorally administered in the autoimmune phase at an interval of 5 days 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kin

10、g AR, et al. Discovery of potent and reversible monoacylglycerol lipase inhibitors. Chem Biol. 2009 Oct 30;16(10):1045-52.2. Deng Q, et al. Pristimerin inhibits angiogenesis in adjuvant-induced arthritic rats by suppressing VEGFR2 signaling pathways. IntImmunopharmacol. 2015 Dec;29(2):302-13.McePdfHeightCaution: Product has not been fully vali