LHVS
目录号: PL08789 纯度: ≥99%
CAS No. :170111-28-1
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中文名称
LHVS
中文别名
N-[(1S)-1-[[(E,1S)-3-(苯磺酰基)-1-苯乙基烯丙基]氨基甲酰基]-3-甲基丁基]吗啉-4-甲酰胺
英文名称
LHVS
英文别名
LHVS
Cas No.
170111-28-1
分子式
C28H37N3O5S
分子量
527.68
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
LHVS 是一种有效的,非选择性的,不可逆的,可透过细胞的半胱氨酸蛋白酶 (cysteine protease) 和组织蛋白酶 (cathepsin) 抑制剂。LHVS 可减少肌动蛋白环的形成。LHVS 抑制 T. gondii 侵袭,其 IC50 为 10 μM。
生物活性
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
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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