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LHVS
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LHVS图片
CAS NO:170111-28-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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-permeablecysteine proteaseandcathepsininhibitor. LHVS decreases actin ring formation. LHVS inhibitsT. gondiiinvasion with anIC50of 10 μM[1][2][3].

IC50& Target

cathepsin S

 

cathepsin K

 

cathepsin L

 

Cathepsin B

 

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[1].
LHVS acts in a dose-dependent manner on osteoclasts and at 5 μM, LHVS inhibits cathepsins K, L, S, and B[1].
LHVS (1-5 nM) can inhibit specifically cathepsin S in HOM2 cells, leaving other cysteine proteases functionally active[3].
LHVS impairs tachyzoite attachment by blocking the release of at least two key invasion proteins, MIC2 and M2AP, from the micronemes[2].
LHVS (50 μM) selectively impairs microneme protein secretion[2].

体内研究
(In Vivo)

LHVS (3-30 mg/kg, SC, once) shows anti-hyperalgesic effect in neuropathic rats[4].
LHVS (30 nmol per rat, spinal delivery, daily) is antinociceptive in neuropathic rats[5].
LHVS (1-50 nmol per rat, Intrathecal injection, daily) reverses established neuropathic mechanical hyperalgesia in 14-day neuropathic rats[5].

Animal Model:Male Wistar rats (180-220 g)[4]
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)[5]
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)[5]
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.
分子量

527.68

性状

Solid

Formula

C28H37N3O5S

CAS 号

170111-28-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(189.51 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8951 mL9.4754 mL18.9509 mL
5 mM0.3790 mL1.8951 mL3.7902 mL
10 mM0.1895 mL0.9475 mL1.8951 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.5 mg/mL (4.74 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.74 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。