TMC114 (Darunavir) | HIV-1 protease inhibitor

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TMC114 (Darunavir) | HIV-1 protease inhibitor

Price:

$169.00

Catalog #:

C8114-5

* Package Size:

5 mg (10 mM solution in DMSO)
5 mg (powder)
25 mg (powder)
100 mg (powder)

Quantity:

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 4^oC desiccated, or store DMSO solution at -20^oC.

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.