计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
Form:Solid
IC50& Target:cathepsin S cathepsin K cathepsin L Cathepsin B
规格
规格或纯度
≥99%
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。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
IUPAC Name
N-[(2R)-1-[[(E,3R)-1-(benzenesulfonyl)-5-phenylpent-1-en-3-yl]amino]-4-methyl-1-oxopentan-2-yl]morpholine-4-carboxamide
INCHI
1S/C28H37N3O5S/c1-22(2)21-26(30-28(33)31-16-18-36-19-17-31)27(32)29-24(14-13-23-9-5-3-6-10-23)15-20-37(34,35)25-11-7-4-8-12-25/h3-12,15,20,22,24,26H,13-14,16-19,21H2,1-2H3,(H,29,32)(H,30,33)/b20-15+/t24-,26-/m1/s1
InChi Key
YUMYYTORLYHUFW-ZUDLOMHPSA-N
Smiles
CC(C)CC(C(=O)NC(CCC1=CC=CC=C1)C=CS(=O)(=O)C2=CC=CC=C2)NC(=O)N3CCOCC3
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
分子量
527.68
技术文档
高级数据
三维结构
交互式化学结构模型
关联靶点（人）
CTSL
Tclin
组织蛋白酶L1(Cathepsin L1)
(3 活性数据)
CTSS
Tchem
组织蛋白酶S(Cathepsin S)
(3 活性数据)
CTSK
Tchem
组织蛋白酶K(Cathepsin K)
(2 活性数据)
CTSB
Tchem
组织蛋白酶B(Cathepsin B)
(1 活性数据)
CTSB
Tchem
Cathepsin B
(3822 活性数据)
CTSG
Tchem
Cathepsin G
(2304 活性数据)
CTSK
Tchem
Cathepsin K
(3011 活性数据)
CTSS
Tchem
Cathepsin S
(3285 活性数据)
CTSH
Tchem
Cathepsin H
(179 活性数据)
CTSC
Tchem
Dipeptidyl peptidase I
(1385 活性数据)
关联靶点（其它种属）
CTSL
Cathepsin L (58 活性数据)
Toxoplasma gondii (4585 活性数据)
Rattus norvegicus (775804 活性数据)
Ctsl
Cathepsin L1 (28 活性数据)
Prtn3
Myeloblastin (11 活性数据)
Elane
Neutrophil elastase (15 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (189.51 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 170111-28-1，分子式为 C28H37N3O5S，分子量为 527.68 g/mol。InChIKey YUMYYTORLYHUFW-ZUDLOMHPSA-N。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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