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L-870810

Cat. No. M41185
L-870810 Structure
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Biological Activity

L-870810 is a potent HIV-1 IN chain transfer inhibitor with antiviral activity.

Chemical Information
Molecular Weight 430.45
Formula C20H19FN4O4S
CAS Number 410544-95-5
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] Melissa S Egbertson. Curr Top Med Chem. HIV integrase inhibitors: from diketoacids to heterocyclic templates: a history of HIV integrase medicinal chemistry at Merck West Point and Merck Rome (IRBM)

[2] Haolun Jin et al. Bioorg Med Chem Lett. Design, synthesis, and SAR studies of novel and highly active tri-cyclic HIV integrase inhibitors

[3] Jacqueline D Reeves et al. Drugs. Emerging drug targets for antiretroviral therapy

[4] M Bayés et al. Methods Find Exp Clin Pharmacol. Gateways to clinical trials

[5] Wade Blair et al. Expert Opin Investig Drugs. 5th Antiviral Drug Discovery and Development Summit

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