• Other

    Other
  • CN

    CN
  • EU

    EU
  • USA

    USA
    • My cart
    In the shopping cart is not goods, to choose and buy!
    • Product Name
    • Size
    • Quantity
    • Amount
      Selected items : 0 pieces Total : CHECK OUT()
      Lopinavir (ABT-378; Kaletra; Aluvia)
      Lopinavir (ABT-378; Kaletra; Aluvia)

      Price：
      Market Price：

      This product is for research use only, not for human use. We do not sell to patients.
      Number： - + Pieces（InventoryPieces）
      InvivoChem Cat #: V0730
      CAS #: 192725-17-0 Purity ≥98%

      Description: Lopinavir (formerly known as ABT-378; trade names Kaletra; Aluvia), an FDA approved antiretroviral drug in 2000 for HIV treatment, is a highly potent HIV protease inhibitor with Ki of 1.3 pM in a cell-free assay. Lopinavir is a ritonavir analog designed to have a diminished interaction with Val82 in HIV protease. It maintains a high potency inhibiting Val82 mutant HIV selected by ritonavir with 50% effective concentration EC50 value lower than 0.06 μM. Although the antiviral activity of ritonavir is considerably attenuated by human serum, lopinavir is less affected by human serum proteins and is 10-fold greater in potency than ritonavir in the presence of human serum. Lopinavir is used in a fixed-dose combination with another protease inhibitor, Ritonavir against HIV infections, and was marketed under the trade names Kaletra and Aluvia. 

      References: Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91.

      Related CAS: 192725-39-6 (Lopinavir Metabolite M1); 357275-54-8 (Lopinavir M-3/M-4)

      Customer Validation
      Official Supplier of
      • VE
      • OF
      • YALE
      • hhmi
      • 香港大学

      详情页公告Product Catalog 2022

      Bulletin Board

      详情页公告Guide to Product Handling


      Publications Citing InvivoChem Products
      • Physicochemical and Storage Information
      • Protocol
      • Quality Control Documentation
      • Related Biological Data
      • Customer Review
      Molecular Weight (MW)628.8
      FormulaC37H48N4O5
      CAS No.192725-17-0
      Storage-20℃ for 3 years in powder form
      -80℃ for 2 years in solvent
      Solubility (In vitro)DMSO: 126 mg/mL (200.4 mM)
      Water: <1 mg/mL
      Ethanol: 126 mg/mL (200.4 mM)
      Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
      SynonymsABT-378; A-157378.0; ABT 378; trade names: Aluviran; Koletra; ABT378; A 157378.0; A157378.0; 

      Chemical Name: (2S)-N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide

      InChi Key: KJHKTHWMRKYKJE-SUGCFTRWSA-N

      InChi Code: InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1

      SMILES Code: CC1=C(C(=CC=C1)C)OCC(=O)N[[email protected]@H](CC2=CC=CC=C2)[[email protected]](C[[email protected]](CC3=CC=CC=C3)NC(=O)[[email protected]](C(C)C)N4CCCNC4=O)O


      • Molarity Calculator
      • Dilution Calculator
      • The molarity calculator equation

        Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

        • Mass
        • Concentration
        • Volume
        • Molecular Weight *
        • =
        • ×
        • ×
      • The dilution calculator equation

        Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

        This equation is commonly abbreviated as: C1V1 = C2V2

        • Concentration (start)
        • ×
        • Volume (start)
        • =
        • Concentration (final)
        • ×
        • Volume (final)
        • ×
        • =
        • ×
        • C1
        •  
        • V1
        •  
        • C2
        •  
        • V2
      In Vitro

      In vitro activity: Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6.

      Kinase Assay: Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM. Target: HIV protease Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. 

      Cell Assay: Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6.  

      In VivoLopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. 
      Animal modelSprague-Dawley-derived rats or cynomolgus monkeys 
      Formulation & DosageDissolved in ethanol-propylene glycol-D5W;10 mg/kg; p.o.
      ReferencesAntimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91.

      These protocols are for reference only. InvivoChem does not independently validate these methods.

       

      Lopinavir

      Mean ± SD plasma ABT-378 levels in healthy human volunteers following administration of a single 400-mg dose. Dashed line, ABT-378 dosed singly; solid line, ABT-378 dosed with 50 mg of ritonavir; dotted line, EC50 of ABT-378 against wild type (WT) HIV in vitro. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.
      		 

      Lopinavir

      Inhibition of the metabolism of ABT-378 and saquinavir by ritonavir in rat and human liver microsomes. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.
      		 

      Lopinavir

      Mean ± standard error of the mean plasma ABT-378 levels after oral dosing with 10 mg/kg singly and in combination with various doses of ritonavir in rats. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.

      评论

        Home Prev Next Last page / pices

        发评论

        ×
        Your information is safe with us. * Required Fields.
        Products are for research use only;  We do not sell to patients
        Contact Us
        Contact Us
        Tel: 1-708-310-1919
        Fax: 1-708-557-7486
        Email: [email protected]
        Frequently Asked Questions
        Subscribe to our E-newsletter
        • Name*
        • *
        • E-mail*
        • *
        • instructions：
        • *
        Copyright 2020 InvivoChem LLC | All Rights Reserved
          Site map
        prompt
        Do you confirm the receipt?