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Lenacapavir sodium

Cat. No. M40754
Lenacapavir sodium Structure
Synonym:

GS-6207 sodium

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Biological Activity

Lenacapavir sodium is a first-in-class, long-acting HIV capsid inhibitor. Lenacapavir sodium has anti-HIV activity with an EC50 of 100 pM in MT-4 cells and an average EC50 of 50 pM (20-160 pM) in peripheral blood mononuclear cells against 23 clinical isolates of HIV-1 from different subtypes.

Chemical Information
Molecular Weight 990.3
Formula C39H31ClF10N7NaO5S2
CAS Number 2189684-44-2 (free base)
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] No authors listed. Am J Health Syst Pharm. Lenacapavir Sodium

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