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 |
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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].
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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. |
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(189.51 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8951 mL | 9.4754 mL | 18.9509 mL | | 5 mM | 0.3790 mL | 1.8951 mL | 3.7902 mL | | 10 mM | 0.1895 mL | 0.9475 mL | 1.8951 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。 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。 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。
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