Indinavir sulfate (MK-639) 是一种口服有效并且具有选择性的HIV-1蛋白酶抑制剂，其对PR的Ki值为 0.54 nM。Indinavir sulfate 可通过抑制基质金属蛋白酶-2 水解的激活，抗血管生成以及促癌细胞凋亡来发挥抗癌活性。Indinavir sulfate 也是一种SARS-CoV 3CLpro抑制剂。
| 生物活性 | Indinavir sulfate (MK-639) is an orally active and selectiveHIV-1proteaseinhibitor with aKiof 0.54 nM forPR. Indinavir sulfate exhibits anticancer activity by inhibiting the activation ofMMPs-2hydrolysis, anti-angiogenesis and inducingapoptosis. Indinavir sulfate is also aSARS-CoV3CLproinhibitor[1][2][3][4]. |
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体外研究
(In Vitro) | Indinavir sulfate (0-50 μM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses[1].
Indinavir sulfate (40 μM-40 nM; 5 days) inhibits cell invasion and (40 μM-40 nM; 48 h) MMPs-2 activation of the Huh7 and SK-HEP-1 hepatocarcinoma cells in vitro[2].
Cell Viability Assay[1] | Cell Line: | PBMCs (from healthy and HIV-infected volunteers) | | Concentration: | 0-50 μM | | Incubation Time: | 18 h (pretreatment; stimulation with anti-CD3 for an additional 48 hours) | | Result: | Blocked anti-CD3-induced cell-cycle progression in a dose-dependent manner.
Resulted in dose-dependent reduction of lymphoproliferative responses. |
Cell Invasion Assay[2] | Cell Line: | Huh7 and SK-HEP-1 cells | | Concentration: | 40 μM-40 nM | | Incubation Time: | 5 days | | Result: | Reduced ability to invade an in vitro constituted extracellular matrix for both cell lines treated compared with the untreated cells. |
Western Blot Analysis[2] | Cell Line: | Huh7 and SK-HEP-1 cells | | Concentration: | 40 μM-40 nM | | Incubation Time: | 48 h | | Result: | Blocked the conversion of latent MMP-2 to its 62/64-kDa active form. |
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体内研究
(In Vivo) | Indinavir sulfate (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo[2].
| Animal Model: | Nude mice(s.c. into Huh7 and SK-HEP-1 cells)[2]. | | Dosage: | 70 mg/kg | | Administration: | Oral gavage; once a day for 3 weeks. | | Result: | Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo. |
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| 中文名称 | 硫酸茚地那韦；硫酸茚地那维；硫酸吲地纳韦；硫酸英地那韦；硫酸印地那韦 |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(140.48 mM) H2O : 50 mg/mL(70.24 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.4048 mL | 7.0238 mL | 14.0475 mL | | 5 mM | 0.2810 mL | 1.4048 mL | 2.8095 mL | | 10 mM | 0.1405 mL | 0.7024 mL | 1.4048 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 (sealed storage, away from moisture)。-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： PBS Solubility: 100 mg/mL (140.48 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.51 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.51 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 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.51 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.51 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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