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Lopinavir

Cat. No. M2158
Lopinavir Structure
Synonym:

ABT-378

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 30  USD30 In stock
50mg USD 50  USD50 In stock
100mg USD 80  USD80 In stock
200mg USD 125  USD125 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 628.8
Formula C37H48N4O5
CAS Number 192725-17-0
Solubility (25°C) DMSO 110 mg/mL
Ethanol 100 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Weemhoff JL, et al. J Pharm Pharmacol. Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir.

[2] Sham HL, et al. Antimicrob Agents Chemother. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease.

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