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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250mg |
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Other Sizes |
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Purity: ≥98%
Fosamprenavir Calcium (Amprenavir phosphate; GW-433908) is a phosphate ester prodrug of Amprenavir with improved solubility. It can be used as an anti-HIV drug. 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 with the IC50 of 0.6 nM on HIV-1 protease, it also weakly inhibits HIV-2 protease with IC50 value of 19 nM. In addition, it is reported to be a Cytochrome P450 3A4 Inhibitor. Amprenavir has been effectively used for the treatment of HIV disease in patients with primary HIV infection. It was approved by the FDA on April 15, 1999, for twice-a-day dosing instead of needing to be taken every eight hours.
ln Vitro |
Fosamprenavir calcium salt (GW433908G), the prodrug's calcium salt, was selected for additional research because it seemed to have the most promise for creating novel drug formulations [1].
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References |
[1]. Falcoz C, et al. Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. J Clin Pharmacol. 2002 Aug;42(8):887-98.
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Molecular Formula |
C25H34CAN3O9PS
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Molecular Weight |
623.67
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CAS # |
226700-81-8
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Related CAS # |
Fosamprenavir;226700-79-4
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(C)CN(C[C@H]([C@H](CC1=CC=CC=C1)NC(=O)O[C@H]2CCOC2)OP(=O)([O-])[O-])S(=O)(=O)C3=CC=C(C=C3)N.[Ca+2]
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InChi Key |
PMDQGYMGQKTCSX-HQROKSDRSA-L
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InChi Code |
InChI=1S/C25H36N3O9PS.Ca/c1-18(2)15-28(39(33,34)22-10-8-20(26)9-11-22)16-24(37-38(30,31)32)23(14-19-6-4-3-5-7-19)27-25(29)36-21-12-13-35-17-21/h3-11,18,21,23-24H,12-17,26H2,1-2H3,(H,27,29)(H2,30,31,32)/q+2/p-2/t21-,23-,24+/m0./s1
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Chemical Name |
calcium[(2R,3S)-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-[[(3S)-oxolan-3-yl]oxycarbonylamino]-4-phenylbutan-2-yl] phosphate
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Synonyms |
Lexiva GW433908G Amprenavir phosphate calcium UNII-ID1GU2627N GW 433908 GW 433908G GW 908 GW-433908 GW-433908G GW-908
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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 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 : ~50 mg/mL (~80.17 mM)
H2O : ~0.25 mg/mL (~0.40 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.01 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 (4.01 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 (4.01 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 | 1.6034 mL | 8.0171 mL | 16.0341 mL | |
5 mM | 0.3207 mL | 1.6034 mL | 3.2068 mL | |
10 mM | 0.1603 mL | 0.8017 mL | 1.6034 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.