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- TMC114 (Darunavir) | HIV-1 protease inhibitor
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- TMC114 (Darunavir) | HIV-1 protease inhibitor
Product Description
Darunavir Ethanolate (TMC114), a phenylalanine mimic, is a potent inhibitor of HIV-1 protease with EC50 activity against the wild type IIIB strain of 4 nM and an average EC50 activity against mutant protease inhibitor strains M1-M5 of 5 nM. [1] Furthermore, fof 150 protease inhibitor-resistant viruses tested, 75% were inhibited by darunavir with a EC50 of
Darunavir exhibits no cytotoxicity at concentrations up to 100 uM and has been shown to be synergistic with a variety of other protease inhibitors and reverse transcriptase inhibitors. [3]
Technical information:
| Chemical Formula: | C27H37N3O7S.C2H5OH | |
| CAS #: | 635728-49-3 | |
| Molecular Weight: | 593.73 | |
| Purity: > 98% | ||
| Appearance: | White | |
| Chemical Name: | N-[(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester compd. with ethanol | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | TMC114, 635728-49-3, Darunavir Ethanolate, Darunavir, Prezista |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Surleraux et al., Discovery and Selection of TMC114, a Next Generation HIV-1 Protease Inhibitor. J. Med. Chem. 2005, 48, 1813-1822. Pubmed ID: 15771427 |
| 2. | Molina et al., Darunavir (TMC114): a new HIV-1 protease inhibitor. Expert Opin. Pharmacother. 2007, 8(12), 1951-1964. Pubmed ID: 17696796 |
| 3. | De Meyer et al., TMC114, a Novel Human Immunodeficiency Virus Type 1 Protease Inhibitor Active against Protease Inhibitor-Resistant Virsues, Including a Broad Range of Clinical Isolates. Antimicrob. Agents. Chemother. 2005, 49(6), 2314-2321. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
