Lopinavir

CHF 45.00
In stock
AG-CR1-3715-M02525 mgCHF 45.00
AG-CR1-3715-M100100 mgCHF 135.00
AG-CR1-3715-M250250 mgCHF 240.00
More Information
Product Details
Synonyms A-157378.0; ABT-378; Aluviran
Product Type Chemical
Properties
Formula

C37H48N4O5

MW 628.8
CAS 192725-17-0
Purity Chemicals ≥98% (1H-NMR)
Appearance White to off-white solid.
Solubility Soluble in ethanol (20mg/ml), DMSO (15mg/ml) or dimtheylformamide (15mg/ml).
InChi Key KJHKTHWMRKYKJE-SUGCFTRWSA-N
Smiles O=C1NCCCN1[C@@H](C(C)C)C(N[C@@H](CC2=CC=CC=C2)C[C@H](O)[C@H](CC3=CC=CC=C3)NC(COC4=C(C)C=CC=C4C)=O)=O
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
  • The antiviral agent Lopinavir is a potent inhibitor of HIV-1 protease (Ki=1.3pM for wild-type enzyme) and has been shown to block the replication of clinical isolates of HIV (EC50s=5-52nM).
  • Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir). Lopinavir/ritonavir inhibits the HIV protease enzyme by forming an inhibitor-enzyme complex thereby preventing cleavage of the gag-pol polyproteins. Immature, non- infectious viral particles are subsequently produced.
  • Lopinavir also has an ability to inhibit ZMPSTE24 (zinc metallopeptidase STE24). HIV-PIs block prelamin A processing by directly affecting the enzymatic activity of ZMPSTE24 and in this way they may contribute to lipodystrophy in individuals undergoing HIV-PI treatment. It also has been shown to inhibit meningioma cell proliferation, induce apoptosis on lymphoma cells and inhibit insulin signaling.
  • Shown in a SARS-CoV-2 protease structure model study to potentially bind and inhibit the coronavirus endopeptidase C30 (CEP_C30) of SARS-CoV-2. A initial randomized trial study was not successful.
Product References
  1. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease: H.L. Sham, et al.; Antimicrob. Agents Chemother. 42, 3218 (1998)
  2. Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir): H.L. Sham, et al.; Bioorg. Med. Chem. Lett. 11, 1351 (2001)
  3. In vitro antiviral interaction of lopinavir with other protease inhibitors: A. Molla, et al.; Antimicrob. Agents Chemother. 46, 2249 (2002)
  4. In vitro hypersusceptibility of human immunodeficiency virus type 1 subtype C protease to lopinavir: L.M. Gonzalez, et al.; Antimicrob. Agents Chemother. 47, 2817 (2003)
  5. Role of lopinavir/ritonavir in the treatment of SARS: initial virological and clinical findings: C.M. Chu, et al.; Thorax 59, 252 (2004)
  6. HIV-protease inhibitors block the enzymatic activity of purified Ste24p: S.E. Hudon, et al.; BBRC 374, 365 (2008)
  7. Lopinavir inhibits meningioma cell proliferation by Akt independent mechanism: M.D. Johnson, et al.; J. Neurooncol. 101, 441 (2011)
  8. HIV protease inhibitor Lopinavir induces apoptosis of primary effusion lymphoma cells via suppression of NF-κB pathway: R. Kariya, et al.; Cancer Lett. 342, 52 (2014)
  9. Lopinavir inhibits insulin signaling by promoting protein tyrosine phosphatase 1B expression: T. Kitazawa, et al.; Exp. Ther. Med. 8, 851 (2014)
  10. A systematic review of lopinavir therapy for SARS coronavirus and MERS coronavirus-A possible reference for coronavirus disease-19 treatment option: T.T. Yao, et al.; J. Med. Virol. (Epub ahead of print) (2020) (Review)
  11. 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)
  12. A Trial of Lopinavir-Ritonavir in Adults Hospitalized with Severe Covid-19: B. Cao, et al.; N. Engl. J. Med. (Epub ahead of print) (2020)
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