| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
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Purity: ≥98%
Indinavir sulfate (IDV; formerly known as MK-639; DRG-0233; L735524; trade name Crixivan), the sulfate salt of indinavir, is a potent and specific HIV protease inhibitor with antiviral effects and good oral bioavailability. Indinavir is used as a component of highly active antiretroviral therapy to treat HIV/AIDS. It is soluble white powder administered orally in combination with other antiviral drugs. The drug prevents protease from functioning normally. Consequently, HIV viruses cannot reproduce, causing a decrease in the viral load. Commercially sold indinavir is indinavir anhydrous, which is indinavir with an additional amine in the hydroxyethylene backbone. This enhances its solubility and oral bioavailability, making it easier for users to intake. It was synthetically produced for the purpose of inhibiting the protease in the HIV virus.
| Targets |
MMP-2;HIV-1
|
|---|---|
| ln Vitro |
Indinavir sulfate (0-50 μM; 18 h) inhibits the G0/G1 phase of the lymphocyte cell cycle in PBMCs and reduces the ability of the cells to proliferate lymphomegaly[1].
In vitro, indinavir sulfate (40 μM–40 nM; 5 days) inhibits Huh7 and SK-HEP-1 hepatocarcinoma cells' ability to invade cells and activate MMPs-2 (40 μM–40 nM; 48 h)[2]. |
| ln Vivo |
Indinavir sulfate (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo[2].
|
| Cell Assay |
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. |
| Animal Protocol |
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. |
| References |
| Molecular Formula |
C36H49N5O8S
|
|---|---|
| Molecular Weight |
711.87
|
| Exact Mass |
711.33
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| Elemental Analysis |
C, 60.74; H, 6.94; N, 9.84; O, 17.98; S, 4.50
|
| CAS # |
157810-81-6
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| Related CAS # |
Indinavir;150378-17-9;Indinavir sulfate ethanolate;2563866-80-6
|
| Appearance |
Solid powder
|
| SMILES |
O=C([C@H]1N(C[C@@H](O)C[C@@H](CC2=CC=CC=C2)C(N[C@@H]3[C@H](O)CC4=C3C=CC=C4)=O)CCN(CC5=CC=CN=C5)C1)NC(C)(C)C.O=S(O)(O)=O
|
| InChi Key |
NUBQKPWHXMGDLP-BDEHJDMKSA-N
|
| InChi Code |
InChI=1S/C36H47N5O4.H2O4S/c1-36(2,3)39-35(45)31-24-40(22-26-12-9-15-37-21-26)16-17-41(31)23-29(42)19-28(18-25-10-5-4-6-11-25)34(44)38-33-30-14-8-7-13-27(30)20-32(33)43;1-5(2,3)4/h4-15,21,28-29,31-33,42-43H,16-20,22-24H2,1-3H3,(H,38,44)(H,39,45);(H2,1,2,3,4)/t28-,29+,31+,32-,33+;/m1./s1
|
| Chemical Name |
(2S)-1-[(2S,4R)-4-benzyl-2-hydroxy-5-[[(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]amino]-5-oxopentyl]-N-tert-butyl-4-(pyridin-3-ylmethyl)piperazine-2-carboxamide sulfate
|
| Synonyms |
trade name: Crixivan; DRG-0233; DRG0233; L-735 524 sulfate; DRG 0233; MK-639 sulfate; L 735 524; MK 639; L735 524; MK639;
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL ( ~140.47 mM )
H2O :~50 mg/mL (~70.24 mM ) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (3.51 mM) Solubility in Formulation 5: 100 mg/mL (140.48 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Protease-inhibitor interactions.J Mol Biol.2005 Dec 9;354(4):789-800. |
The catalytic site of PRL24I–p2/NC at 1.1 Å resolution.J Mol Biol.2005 Dec 9;354(4):789-800. |
Structural differences at sites of mutation.J Mol Biol.2005 Dec 9;354(4):789-800. |
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