Darunavir_product_DataBase

Bioactivity

Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity[1][2].

Invitro

Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors[1].Darunavir (TMC114, UIC-94017) blocks the infectivity and replication of each of HIV-1NL4-3 variants exposed to and selected for resistance to Ro 31-8959, MK-639, AG1341, or ABT 538 at concentrations up to 5 μM (IC50s, 0.003 to 0.029 μM), although it was less active against HIV-1NL4-3 variants selected for resistance to VX-478 (IC50, 0.22 μM)[2].

Name

Darunavir

CAS

206361-99-1

Formula

C27H37N3O7S

Molar Mass

547.66

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Dominique L N G Surleraux, et al. Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor. J Med Chem. 2005 Mar 24;48(6):1813-22. [2]. Yasuhiro Koh, et al. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro. Antimicrob Agents Chemother. 2003 Oct;47(10):

PeptideDB

Darunavir

CAS: 206361-99-1 F: C27H37N3O7S W: 547.66