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10-029

Lopinavir

ProSci

DESCRIPTION

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.

DETAILS

  • Cas: 192725-17-0
  • Purity: greater than or equal to 98% (1H-NMR)
  • 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
  • Formula: C37H48N4O5
  • Storage: Short Term Storage: +4C. Long Term Storage: -20C. Handling Advice: Keep cool and dry. Use/Stability: Stable for at least 2 years after receipt when stored at -20C.
  • Shipping: Room Temp
  • Inchi Key: KJHKTHWMRKYKJE-SUGCFTRWSA-N
  • Solubility: Soluble in DMSO, methanol or ethanol. Insoluble in water.
  • Physical State: Lyophilized
  • Additional Names: A-157378.0; ABT-378; Aluviran
  • Predicted Molecular Weight: 628.8