LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC 50 of 10 μM.
性状
Solid
IC50 & Target[1][2]
cathepsin S cathepsin K
体外研究(In Vitro)
LHVS (5 μM, 2 h) results in a 50% reduction of actin ring formation in wild-type osteoclasts when compared with untreated osteoclasts.LHVS acts in a dose-dependent manner on osteoclasts and at 5 μM, LHVS inhibits cathepsins K, L, S, and B.LHVS (1-5 nM) can inhibit specifically cathepsin S in HOM2 cells, leaving other cysteine proteases functionally active.LHVS impairs tachyzoite attachment by blocking the release of at least two key invasion proteins, MIC2 and M2AP, from the micronemes.LHVS (50 μM) selectively impairs microneme protein secretion. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
LHVS (3-30 mg/kg, SC, once) shows anti-hyperalgesic effect in neuropathic rats.
LHVS (30 nmol per rat, spinal delivery, daily) is antinociceptive in neuropathic rats.
LHVS (1-50 nmol per rat, Intrathecal injection, daily) reverses established neuropathic mechanical hyperalgesia in 14-day neuropathic rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wilson SR, et al. Cathepsin K activity-dependent regulation of osteoclast actin ring formation and bone resorption. J Biol Chem. 2009 Jan 23;284(4):2584-92.[2]. Teo CF, et al.Cysteine protease inhibitors block Toxoplasma gondii microneme secretion and cell invasion. Antimicrob Agents Chemother. 2007 Feb;51(2):679-88.
溶解度数据
In Vitro: DMSO : 100 mg/mL (189.51 mM; Need ultrasonic)配制储备液