Darunavir . ethanolate

CHF 70.00
In stock
AG-CR1-3724-M01010 mgCHF 70.00
AG-CR1-3724-M05050 mgCHF 210.00
AG-CR1-3724-M250250 mgCHF 520.00
More Information
Product Details
Synonyms TMC114; TMC41629; UIC-94017; HSDB 7788; Prezista
Product Type Chemical
Properties
Formula

C27H37N3O7S . C2H5OH

MW 547.7 . 46.0
CAS 635728-49-3
Purity Chemicals ≥98% (HPLC)
Appearance White to off-white solid.
Solubility Soluble in DMSO (30mg/ml). Very slightly soluble in water (~0.15mg/ml).
Identity Determined by 1H-NMR.
InChi Key QWSHKNICRJHQCY-VBTXLZOXSA-N
Smiles NC1=CC=C(S(=O)(N(C[C@@H](O)[C@H](CC2=CC=CC=C2)NC(O[C@H]3CO[C@]4([H])[C@@]3([H])CCO4)=O)CC(C)C)=O)C=C1.CCO
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage -20°C
Handling Advice Keep cool and dry.
Use/Stability Stable for at least 2 years after receipt when stored at -20°C.
Documents
MSDS Download PDF
Product Specification Sheet
Datasheet Download PDF
  • Darunavir ethanolate is a highly potent HIV protease inhibitor (IC50=3-6nM, depending on laboratory HIV-1 strain), an antiretroviral medication used to treat and prevent HIV/AIDS. The ethanolate formulation has some stability advantages compared to the free base Darunavir (Prod. No. AG-CR1-3712).
  • Darunavir ethanolate is a second generation HIV-1 protease inhibitor that inhibits replication of various laboratory strains and clinical isolates of HIV-1, including those resistant to first generation protease inhibitors. It inhibits cell-free diffusion and cell-to-cell spread of HIV-1 in Jurkat cell populations.
  • Formulations containing darunavir have been used in combination therapy for the treatment of HIV.
  • Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the papain like viral protease (PLVP) of SARS-CoV-2, responsible for COVID-19.
Product References
  1. Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere: A.K. Ghosh, et al.; Bioorg. Med. Chem. Lett. 8, 687 (1998)
  2. Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro: Y. Koh, et al.; Antimicrob. Agents Chemother. 47, 3123 (2003)
  3. Darunavir: a second-generation protease inhibitor: K.H. Busse & S.R. Penzak; Am. J. Health Syst. Pharm. 64, 1593 (2007) (Review)
  4. Darunavir (TMC114): a new HIV-1 protease inhibitor: J.M. Molina & A. Hill; Expert. Opin. Pharmacother. 8, 1951 (2007) (Review)
  5. Darunavir: a nonpeptidic antiretroviral protease inhibitor: C. McCoy; Clin. Ther. 29, 1559 (2007) (Review)
  6. Protease inhibitors effectively block cell-to-cell spread of HIV-1 between T cells: B.K. Titanji, et al.; Retrovirology 10, 161 (2013)
  7. Polymorphic stability of darunavir and its formulation : J. Chaves, et al.; J. Therm. Anal. Calorim. 123, 2185 (2016)
  8. Molecular Modeling Evaluation of the Binding Effect of Ritonavir, Lopinavir and Darunavir to Severe Acute Respiratory Syndrome Coronavirus 2 Proteases: S. Lin, et al.; (Epub ahead of print) (2020)
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