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5mg |
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10mg |
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50mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Darunavir (also known as TMC114; DRV, Trade name: Prezista among others) is a nonpeptidic HIV protease inhibitor and an antiretroviral medication used to treat and prevent HIV/AIDS. Darunavir was approved by FDA in 2006 to treat and prevent HIV/AIDS infection. In order to treat and prevent HIV/AIDS infection, the FDA approved darunavir in 2006. For adults and adolescents who have never received treatment before as well as those who have, darunavir is a recommended course of action by the Office of AIDS Research Advisory Council. It bears the name of Arun K. Ghosh, a chemist at the University of Illinois at Chicago who made the molecule's discovery and is currently a professor at Purdue University. It was created by the pharmaceutical company Tibotec. Darunavir is typically advised to be used in combination with other antiretrovirals; for instance, to raise levels of darunavir, it is frequently used in conjunction with low dosages of cobicistat or ritonavir. After a needlestick injury or other possible exposure, it might be used as a preventative measure. It is consumed orally once or twice daily.
ln Vitro |
Darunavir (TMC114, 1a) is similar to other protease inhibitors in terms of stability[1].
Darunavir (TMC114, UIC-94017) suppresses the infectivity and replication of all HIV-1NL4-3 variants exposed to and selected for resistance to AG1341, Ro 31-8959, MK-639, or ABT 538 at concentrations as high as 5 μM (IC50s, 0.003 to 0.029 μM), though its effectiveness against variants of HIV-1NL4-3 selected for resistance to VX-478 was lower (IC50, 0.22 μM)[2]. |
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ln Vivo |
Darunavir has a 37% oral bioavailability and is effective against both PI-resistant and wild-type HIV. In conjunction with ritonavir, it is frequently used to increase the bioavailability to 82%.
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Enzyme Assay |
Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
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Cell Assay |
Darunavir has been shown to have higher potency than saquinavir, amprenavir, nelfinavir, indinavir, lopinavir, and ritonavir in an in vitro study using MT-2 cells. The main hepatic cytochrome P450 (CYP) enzyme responsible for darunavir metabolism is CYP3A. The "boosting" dose of ritonavir increases the bioavailability of darunavir by inhibiting CYP3A.
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Animal Protocol |
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References |
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Molecular Formula |
C27H37N3O7S
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Molecular Weight |
547.660
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Exact Mass |
547.24
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Elemental Analysis |
C, 59.21; H, 6.81; N, 7.67; O, 20.45; S, 5.85
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CAS # |
206361-99-1
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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]2CO[C@@H]3[C@H]2CCO3)O)S(=O)(=O)C4=CC=C(C=C4)N
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InChi Key |
CJBJHOAVZSMMDJ-HEXNFIEUSA-N
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InChi Code |
InChI=1S/C27H37N3O7S/c1-18(2)15-30(38(33,34)21-10-8-20(28)9-11-21)16-24(31)23(14-19-6-4-3-5-7-19)29-27(32)37-25-17-36-26-22(25)12-13-35-26/h3-11,18,22-26,31H,12-17,28H2,1-2H3,(H,29,32)/t22-,23-,24+,25-,26+/m0/s1
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Chemical Name |
[(3aS,4R,6aR)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl] N-[(2S,3R)-4-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-hydroxy-1-phenylbutan-2-yl]carbamate
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Synonyms |
Darunavir; TMC-114; TMC114; TMC 114; UIC-94017; UIC 94017; UIC94017; Trade name: Prezista
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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 |
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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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.8260 mL | 9.1298 mL | 18.2595 mL | |
5 mM | 0.3652 mL | 1.8260 mL | 3.6519 mL | |
10 mM | 0.1826 mL | 0.9130 mL | 1.8260 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.