Darunavir

SKU: orb1225723

Description

A potent, selective HIV-1 protease inhibitor that is extremely potent against laboratory HIV-1 strains and primary clinical isolates with IC50 of 3 nM, IC90 of 9 nM; blockes the infectivity and replication of HIV-1(NL4-3) variants with IC50 of 3-29 nM, also potent against multi-PI-resistant clinical HIV-1 variants isolated from patients; used to treat and prevent HIV/AIDS.HIV Infection Approved(In Vitro):Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors.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).

Key Properties

• CAS Number: 206361-99-1
• MW: 547.6636
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₇N₃O₇S
• 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
• Target: HIV
• Solubility: 10 mM in DMSO

Bioactivity

• In Vitro:
  Darunavir (TMC114, 1a) has a stability comparable to other protease inhibitors. 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TMC-114 | UIC-94017

Quick Database Links

Gene Symbol

HIV