| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Amprenavir (formerly VX-478; trade name Agenerase and Prozei), an FDA approved drug for treating HIV infections, is a potent PXR-selective agonist and an HIV protease inhibitor. Its IC50 value for HIV-1 protease is 0.6 nM, and its IC50 value for HIV-2 protease is 19 nM. It is also said to be an inhibitor of cytochrome P450 3A4. Patients with primary HIV infection can benefit from the effective treatment of HIV disease with amprenavir. On April 15, 1999, the FDA approved a twice-daily dose for it, as opposed to an eight-hour interval.
| Targets |
PXR; HIV protease (IC50 = 14.6 ng/mL)
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| ln Vitro |
Amprenavir has an enzyme inhibition constant (Ki = 0.6 nM) that is within the other protease inhibitors' Ki range. The in vitro 50% inhibitory concentration (IC50) of amprenavir against clinical HIV isolates of wild type is 14.6 +/- 12.5 ng/mL (mean +/- SD) [1]. By preventing MMP proteolytic activation, amprenavir directly inhibited the invasion of Huh-7 hepatocarcinoma cell lines [2].
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| ln Vivo |
Amprenavir was able to encourage the remission of hepatocarcinoma growth in vivo through anti-angiogenetic and general anti-tumor activities, through independent pathways related to PI3K/AKT, which is currently one of the more plausible theories to explain the anti-tumor effects of the various protease inhibitors[2]. PXR was effectively activated and PXR target gene expression was induced both in vitro and in vivo by amprenavir. In mice of the wild type, but not in mice lacking PXR, a brief exposure to amprenavir markedly raised the levels of atherogenic low-density lipoprotein cholesterol and plasma total cholesterol [3]. The recommended dosage of amprenavir for adults and children is 1200 mg twice daily for adults, 20 mg/kg twice daily for children under the age of 13, or 15 mg/kg three times daily for adolescents under the weight of 50 kg[1].
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| Cell Assay |
Amprenavir induced the expression of the PXR target gene in LS180 intestinal cells and HepaRG hepatoma cells.
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| Animal Protocol |
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| References |
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| Molecular Formula |
C25H35N3O6S
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| Molecular Weight |
505.63
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| Exact Mass |
505.22
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| Elemental Analysis |
C, 59.39; H, 6.98; N, 8.31; O, 18.99; S, 6.34
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| CAS # |
161814-49-9
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| Related CAS # |
Amprenavir-d4;1217661-20-5;Amprenavir-d4-1;2738376-78-6
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| Appearance |
Solid powder
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| SMILES |
CC(C)CN(C[C@H]([C@H](CC1=CC=CC=C1)NC(=O)O[C@H]2CCOC2)O)S(=O)(=O)C3=CC=C(C=C3)N
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| InChi Key |
YMARZQAQMVYCKC-OEMFJLHTSA-N
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| InChi Code |
InChI=1S/C25H35N3O6S/c1-18(2)15-28(35(31,32)22-10-8-20(26)9-11-22)16-24(29)23(14-19-6-4-3-5-7-19)27-25(30)34-21-12-13-33-17-21/h3-11,18,21,23-24,29H,12-17,26H2,1-2H3,(H,27,30)/t21-,23-,24+/m0/s1
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| Chemical Name |
[(3S)-oxolan-3-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
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| Synonyms |
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| 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 |
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| 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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.94 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 (4.94 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 (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9777 mL | 9.8887 mL | 19.7773 mL | |
| 5 mM | 0.3955 mL | 1.9777 mL | 3.9555 mL | |
| 10 mM | 0.1978 mL | 0.9889 mL | 1.9777 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00002417 | Completed | Drug: Amprenavir | HIV Infections | Glaxo Wellcome | Not Applicable | |
| NCT00002205 | Completed | Drug: Abacavir sulfate Drug: Amprenavir |
HIV Infections | Glaxo Wellcome | Not Applicable | |
| NCT00038519 | Completed | Drug: Amprenavir/ritonavir Drug: Saquinavir/ritonavir |
HIV Infections | Abbott | April 2001 | Phase 2 Phase 3 |
| NCT00002245 | Completed | Drug: Amprenavir Drug: Lamivudine |
HIV Infections | Glaxo Wellcome | April 1999 | Phase 3 |
| NCT00001758 | Completed | Drug: Abacavir Drug: Amprenavir |
HIV Infection | National Institute of Allergy and Infectious Diseases (NIAID) |
August 2003 | Phase 2 |
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