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Lopinavir

Cat. No. M2158
Lopinavir Structure
Synonym:

ABT-378

Size Price Availability Quantity
50mg USD 55 In stock
100mg USD 98 In stock
250mg USD 198 In stock
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Biological Activity

Lopinavir (ABT-378) is an antiretroviral of the protease inhibitor class. Lopinavir potently inhibited wild-type and mutant HIV protease (Ki = 1.3 to 3.6 pM). Lopinavir (ABT-378) also produced negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6. Lopinavir (ABT-378) blocked the replication of laboratory and clinical strains of HIV type 1 (50% effective concentration [EC50], 0.006 to 0.017 microM), and maintained high potency against mutant HIV selected by ritonavir in vivo (EC50, 50-fold after 8 h.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 628.8
Formula C37H48N4O5
CAS Number 192725-17-0
Purity >99%
Solubility DMSO 100 mg/mL
Ethanol 100 mg/mL
Storage at -20°C
References

Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir.
Weemhoff JL, et al. J Pharm Pharmacol. 2003 Mar;55(3):381-6. PMID: 12724045.

ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.
Sham HL, et al. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24. PMID: 9835517.

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Abmole Inhibitor Catalog 2017




Keywords: Lopinavir, ABT-378 supplier, HIV Protease, inhibitors

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