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GSK2838232 

Cat. No. M28448
GSK2838232  Structure
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Biological Activity

GSK2838232 inhibit HIV reverse transcriptase activity across a broad panel of HIV-1 isolates.

Chemical Information
Molecular Weight 809.56
Formula C48H73ClN2O6
CAS Number 1443460-91-0
Form Solid
Solubility (25°C) DMSO ≥ 50 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] Robert A Smith, et al. PLoS One. Intrinsic resistance of HIV-2 and SIV to the maturation inhibitor GSK2838232

[2] Julia L Shamshina, et al. Int J Mol Sci. Are Myths and Preconceptions Preventing us from Applying Ionic Liquid Forms of Antiviral Medicines to the Current Health Crisis?

[3] Mark Johnson, et al. Clin Pharmacol Drug Dev. A Phase 1 Study to Assess the Relative Bioavailability, Food Effect, and Safety of a Tablet Formulation of GSK2838232, a Novel HIV Maturation Inhibitor in Healthy Participants After Single and Repeated Doses

[4] Edwin DeJesus, et al. Clin Infect Dis. A Phase IIa Study Evaluating Safety, Pharmacokinetics, and Antiviral Activity of GSK2838232, a Novel, Second-generation Maturation Inhibitor, in Participants With Human Immunodeficiency Virus Type 1 Infection

[5] Mark Johnson, et al. Pharmacol Res Perspect. The safety, tolerability, and pharmacokinetic profile of GSK2838232, a novel 2nd generation HIV maturation inhibitor, as assessed in healthy subjects

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Keywords: GSK2838232  supplier, HIV Protease, inhibitors, activators

 
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