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Indinavir sulfate/硫酸茚地那韦 {[allProObj[0].p_purity_real_show]}

货号：A290622 同义名： MK-639; L735524

Indinavir sulfate是一种口服有效的 HIV-1 蛋白酶抑制剂，PR 的 Ki 值为 0.54 nM。具有抗血管生成及抗癌作用，同时抑制 SARS-CoV 3CLpro，显示出多领域活性。

Indinavir sulfate/硫酸茚地那韦 化学结构 CAS号：157810-81-6
Indinavir sulfate/硫酸茚地那韦 化学结构
CAS号：157810-81-6
Indinavir sulfate/硫酸茚地那韦 3D分子结构
CAS号：157810-81-6
Indinavir sulfate/硫酸茚地那韦 化学结构 CAS号：157810-81-6
Indinavir sulfate/硫酸茚地那韦 3D分子结构 CAS号：157810-81-6
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Indinavir sulfate/硫酸茚地那韦 纯度/质量文件 产品仅供科研

货号：A290622 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 MMP ↓ 其他靶点 纯度
Marimastat +++

MMP-14, IC50: 3 nM

MMP-7, IC50: 16 nM

 		98%
Ilomastat ++++

MMP-26, Ki: 0.36 nM

MMP-2, Ki: 0.1 nM

 		99%+
SB-3CT +

MMP-9, Ki: 600 nM

MMP-2, Ki: 13.9 nM

 		99%+
Doxycycline ✔ 95%
NSC 405020 ✔ 98%
Batimastat +++

MMP-1, IC50: 3 nM

MMP-7, IC50: 4 nM

 		99%+
Nobiletin ✔ 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
产品名称 HIV Protease ↓ HIV-1 caspid ↓ 其他靶点 纯度
Dextran sulfate sodium salt(MW 40000) ✔ M.W 40000
Vicriviroc maleate ✔ 95%
Rosamultin ✔ 97%
Darunavir ✔ 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

 		99+%
Chloroquine ✔ Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

 		PXR 99%+
NBD-556 ✔ 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

 		99%+
Atazanavir Sulfate ✔ 98%
Limonin ✔ 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

 		98%
Ritonavir ✔ 98%
Azvudine ✔ 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

 		97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Indinavir sulfate/硫酸茚地那韦 生物活性

描述 Indinavir sulfate is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.

Indinavir sulfate/硫酸茚地那韦 细胞实验

Cell Line
Concentration Treated Time Description References
Human brain microvascular endothelial cells (HBMEC) 0.1 mM 2 hours To evaluate the cytotoxicity of indinavir sulfate nanoformulations on HBMEC. Results showed that at 0.1 mM concentration, indinavir sulfate nanoformulations induced little or no HBMEC toxicities. Int J Nanomedicine. 2012;7:2373-88.
Mouse islets 2.1 μmol/l (IC50) 10 minutes To assess the inhibitory effect of indinavir sulfate on glucose-stimulated insulin release. Results showed that indinavir sulfate significantly inhibited insulin release from mouse islets with an IC50 of 2.1 μmol/l. Diabetes. 2003 Jul;52(7):1695-1700.
MIN6 cells 20 μmol/l 5-30 seconds To assess the inhibitory effect of indinavir sulfate on 3-O-methylglucose uptake. Results showed that 20 μmol/l indinavir sulfate significantly delayed 3-O-methylglucose uptake. Diabetes. 2003 Jul;52(7):1695-1700.
RAW 264.7 cells 2 µg/ml 1 hour To determine the effect of indinavir sulfate on RANKL-induced Akt signaling, results showed that indinavir sulfate inhibits RANKL-induced Akt phosphorylation. J Clin Invest. 2004 Jul;114(2):206-13.
Bone marrow macrophages 10 µg/ml 4 days To determine the effect of indinavir sulfate on osteoclast differentiation, results showed that indinavir sulfate does not affect osteoclast formation. J Clin Invest. 2004 Jul;114(2):206-13.
GL261 murine glioblastoma cells >500 μM 24 hours Determine the IC50 of IDV on cell proliferation, found that IDV at concentrations higher than 500 μM had less than 50% inhibition on GL261 cell proliferation Neoplasia. 2017 Apr;19(4):364-373.
U87MG human glioblastoma cells 500 μM 24 hours Determine the IC50 of IDV on cell proliferation, found that IDV at 500 μM inhibited U87MG cell proliferation by 50% Neoplasia. 2017 Apr;19(4):364-373.

Indinavir sulfate/硫酸茚地那韦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Mdr1a knockout mice Intravenous and oral 1.5 mg/kg (intravenous) and 6 mg/kg (oral) Single dose, measured at 4 hours post-administration To study the effect of P-glycoprotein on the oral absorption and brain penetration of indinavir sulfate. Results showed that in mdr1a (?/?) mice, plasma concentrations were elevated 2–5-fold after oral administration, and brain concentrations were elevated 7–36-fold after intravenous administration, indicating that P-glycoprotein limits the oral bioavailability and brain penetration of indinavir sulfate. J Clin Invest. 1998 Jan 15;101(2):289-94
Wistar rats Hyperglycemic clamp model Intravenous infusion 0.5 mg/kg/min Continuous infusion for 120 minutes To assess the effect of indinavir sulfate on β-cell function. Results showed that indinavir sulfate significantly suppressed the first-phase insulin response in rats. Diabetes. 2003 Jul;52(7):1695-1700.
Mice PTH-induced osteoclastogenesis model Intraperitoneal injection 1 mg Twice daily for 3 days To determine the effect of indinavir sulfate on PTH-induced osteoclastogenesis in vivo, results showed that indinavir sulfate completely abrogated PTH-induced osteoclast formation. J Clin Invest. 2004 Jul;114(2):206-13.
Sprague-Dawley rats Hyperinsulinemic-hypoglycemic clamp model Third ventricle infusion 10 mg/min Started 3 hours before and continued throughout the clamp To assess the role of brain GLUT4 in the counterregulatory response to hypoglycemia. Results showed that IDV-treated rats had attenuated epinephrine, norepinephrine, and glucagon responses during hypoglycemia, indicating that GLUT4 plays a critical role in brain glucose sensing and the counterregulatory response to hypoglycemia. Diabetes. 2017 Mar;66(3):587-597
Mice Transgenic mouse model Oral gavage 0.9 mg/day Once daily for 3 or 10 weeks To evaluate the effects of indinavir sulfate in combination with other antiretroviral drugs on cardiac mitochondrial DNA and function. Results showed long-term treatment led to left ventricle hypertrophy and cardiomyopathy. Lab Invest. 2009 Feb;89(2):122-30

Indinavir sulfate/硫酸茚地那韦 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00002440 HIV Infections Phase 2 Completed - United States, California ... 展开 >> UCSD Treatment Ctr San Diego, California, United States, 921036329 United States, Connecticut Yale U / New Haven Med Ctr / AIDS Clinical Trials Unit New Haven, Connecticut, United States, 065102483 United States, Missouri Kansas City AIDS Research Consortium Kansas City, Missouri, United States, 64111 United States, New York NYU Med Ctr / Dept of Medicine / AIDS Clinical Trial New York, New York, United States, 10016 United States, North Carolina Carolinas Med Ctr Charlotte, North Carolina, United States, 28232 United States, Ohio Case Western Reserve Univ / AIDS Clinical Trials Unit Cleveland, Ohio, United States, 44106 United States, Pennsylvania Univ of Pittsburgh Med Ctr Pittsburgh, Pennsylvania, United States, 15213 United States, Tennessee Vanderbilt Univ Med Ctr Nashville, Tennessee, United States, 372321302 收起 <<
NCT00006154 HIV Infections Phase 3 Completed - Canada, British Columbia ... 展开 >> Viridae Clinical Sciences / University of British Columbia Vancouver, British Columbia, Canada Canada, Quebec Centre de traitment d'immunodeficience Montreal, Quebec, Canada Centre Hospitalier de la Universite de Montreal (CHUM) Montreal, Quebec, Canada Institut Thoracique de Montreal Montreal, Quebec, Canada 收起 <<
NCT00000923 HIV Infections Not Applicable Completed - United States, Alabama ... 展开 >> Alabama Therapeutics CRS Birmingham, Alabama, United States, 35294 United States, California USC CRS Los Angeles, California, United States, 900331079 Harbor-UCLA Med. Ctr. CRS Torrance, California, United States, 90502 United States, Hawaii Univ. of Hawaii at Manoa, Leahi Hosp. Honolulu, Hawaii, United States, 96816 United States, Iowa Univ. of Iowa Healthcare, Div. of Infectious Diseases Iowa City, Iowa, United States, 52242 United States, Louisiana Tulane Univ. A1701 CRS New Orleans, Louisiana, United States, 70112 United States, Missouri St. Louis ConnectCare, Infectious Diseases Clinic St Louis, Missouri, United States, 63112 Washington U CRS St. Louis, Missouri, United States United States, New York Mt. Sinai Med. Ctr. A0404 CRS New York, New York, United States, 10029 United States, Ohio Case CRS Cleveland, Ohio, United States, 44106 The Ohio State Univ. AIDS CRS Columbus, Ohio, United States, 432101228 United States, Washington University of Washington AIDS CRS Seattle, Washington, United States, 98104 收起 <<

Indinavir sulfate/硫酸茚地那韦 参考文献

[1]Liu F, Boross PI, et al. Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol. 2005 Dec 9;354(4):789-800.

[2]Stein DS, Fish DG, et al. A 24-week open-label phase I/II evaluation of the HIV protease inhibitor MK-639(indinavir). AIDS. 1996 May;10(5):485-92.

Indinavir sulfate/硫酸茚地那韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.40mL

0.28mL

0.14mL

7.02mL

1.40mL

0.70mL

14.05mL

2.81mL

1.40mL

Indinavir sulfate/硫酸茚地那韦 技术信息

CAS号157810-81-6
分子式C36H49N5O8S
分子量 711.87
SMILES Code O=C([C@@H](C[C@H](O)CN(CCN(CC1=CN=CC=C1)C2)[C@@H]2C(NC(C)(C)C)=O)CC3=CC=CC=C3)N[C@H]4C(C=CC=C5)=C5C[C@H]4O.O=S(O)(O)=O
MDL No. MFCD00920346
别名 MK-639; L735524; Indinavir (sulfate); Crixivan
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

DMSO: 105 mg/mL(147.5 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(70.24 mM)，配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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。
方案 一

Tags: Indinavir | 157810-81-6 | MK-639 | L735524 | MK639 | MK 639 | HIV Protease Inhibitor | Anti-infection | Metabolic Enzyme/Protease | Apoptosis | HIV | HIV Protease | SARS-CoV | Apoptosis | MMP | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Indinavir sulfate/硫酸茚地那韦 纯度/质量文件 | Indinavir sulfate/硫酸茚地那韦 亚型比较 | Indinavir sulfate/硫酸茚地那韦 生物活性 | Indinavir sulfate/硫酸茚地那韦 临床数据 | Indinavir sulfate/硫酸茚地那韦 参考文献 | Indinavir sulfate/硫酸茚地那韦 实验方案 | Indinavir sulfate/硫酸茚地那韦 技术信息

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