产品
编 号：F615522
分子式：C28H37N3O5S
分子量：527.68
分子式：C28H37N3O5S
分子量：527.68
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 170111-28-1
产品详情
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 IC50 of 10 μM.
体内研究：
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.Animal Model:Male Wistar rats (180-220 g)
Dosage:3-30 mg/kg
Administration:SC, once
Result:Produced a dose-dependent reversal of the mechanical hyperalgesia which lasted up to 3 h in neuropathic rats. In contrast, a single systemic administration of LHVS did not reverse mechanical allodynia in neuropathic rats.
Animal Model:Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)
Dosage:30 nmol per rat
Administration:Spinal delivery, Daily
Result:Failed to prevent the development of allodynia when continuous delivery from day 0 to day 7 post-PNL, but significantly reversed allodynia on day 7 post-PNL. In addition, the delivery of LHVS from day 7 to day 14 post-PNL significantly reversed established mechanical allodynia from day 8.
Animal Model:Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)
Dosage:1, 10 or 50 nmol per rat
Administration:Intrathecal injection, Daily
Result:Reduced established mechanical hyperalgesia. This effect was dose-dependent and remained significant until 3 h after administration of the highest dose.
体外研究：
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.
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 IC50 of 10 μM.
体内研究：
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.Animal Model:Male Wistar rats (180-220 g)
Dosage:3-30 mg/kg
Administration:SC, once
Result:Produced a dose-dependent reversal of the mechanical hyperalgesia which lasted up to 3 h in neuropathic rats. In contrast, a single systemic administration of LHVS did not reverse mechanical allodynia in neuropathic rats.
Animal Model:Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)
Dosage:30 nmol per rat
Administration:Spinal delivery, Daily
Result:Failed to prevent the development of allodynia when continuous delivery from day 0 to day 7 post-PNL, but significantly reversed allodynia on day 7 post-PNL. In addition, the delivery of LHVS from day 7 to day 14 post-PNL significantly reversed established mechanical allodynia from day 8.
Animal Model:Male Wistar rats received a partial ligation of the left sciatic nerve (PNL)
Dosage:1, 10 or 50 nmol per rat
Administration:Intrathecal injection, Daily
Result:Reduced established mechanical hyperalgesia. This effect was dose-dependent and remained significant until 3 h after administration of the highest dose.
体外研究：
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.
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