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LHVS

    级别和纯度:
  • 10mM in DMSO
  • CAS编号: 170111-28-1
  • 分子式: C28H37N3O5S
  • 分子量: 527.68
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库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
L655138-1ml
1ml 期货 Stock Image

基本描述

规格或纯度 10mM in DMSO
英文名称 LHVS
生化机理 LHVS 是一种强效、非选择性、不可逆、细胞渗透性半胱氨酸蛋白酶和酪蛋白酶抑制剂。LHVS 可减少肌动蛋白环的形成。LHVS 可抑制淋球菌入侵,其 IC 50 为 10 μM。
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍


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

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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.

IC50& Target:cathepsin S cathepsin K cathepsin L Cathepsin B

关联靶点(人)

CTSL Tclin 组织蛋白酶L1(Cathepsin L1) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CTSS Tchem 组织蛋白酶S(Cathepsin S) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CTSK Tchem 组织蛋白酶K(Cathepsin K) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
CTSB Tchem 组织蛋白酶B(Cathepsin B) (0 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Isomeric SMILES CC(C)C[C@H](C(=O)N[C@H](CCC1=CC=CC=C1)/C=C/S(=O)(=O)C2=CC=CC=C2)NC(=O)N3CCOCC3
PubChem CID 23648296
分子量 527.68

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