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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Indinavir (IDV; formerly DRG-0233; MK639 and L-735524; Crixivan) is an inhibitor of HIV protease approved for use 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 |
HIV-1
MMP-2 |
|---|---|
| ln Vitro |
Indinavir (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 [1].
Huh7 and SK-HEP-1 hepatocarcinoma cells' cell invasion and MMPs-2 activation are inhibited in vitro by indinavir (40 µM–40 nM; 5 days) and 40 µM–40 nM (48 h) respectively[2]. |
| ln Vivo |
Indinavir (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: Compared to placebo, delayed the growth of s.c. implanted hepatocarcinoma xenografts in naked mice. |
| References |
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| Molecular Formula |
C36H47N5O4
|
|---|---|
| Molecular Weight |
613.79
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| Exact Mass |
613.36
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| Elemental Analysis |
C, 70.45; H, 7.72; N, 11.41; O, 10.43
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| CAS # |
150378-17-9
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| Related CAS # |
Indinavir sulfate;157810-81-6;Indinavir sulfate ethanolate;2563866-80-6;Indinavir-d6;185897-02-3
|
| 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
|
| InChi Key |
CBVCZFGXHXORBI-PXQQMZJSSA-N
|
| InChi Code |
InChI=1S/C36H47N5O4/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/h4-15,21,28-29,31-33,42-43H,16-20,22-24H2,1-3H3,(H,38,44)(H,39,45)/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
|
| Synonyms |
trade name: Crixivan; DRG-0233; L-735 524; DRG0233; MK-639; L 735 524; MK 639; DRG 233; 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 |
| 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) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6292 mL | 8.1461 mL | 16.2922 mL | |
| 5 mM | 0.3258 mL | 1.6292 mL | 3.2584 mL | |
| 10 mM | 0.1629 mL | 0.8146 mL | 1.6292 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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