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GCA-186 

Cat. No. M28543
GCA-186  Structure
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Biological Activity

GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively.

Chemical Information
Molecular Weight 330.42
Formula C19H26N2O3
CAS Number 149950-61-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Nasser R El-Brollosy, et al. Arch Pharm (Weinheim). Synthesis and antiviral evaluation of 6-(trifluoromethylbenzyl) and 6-(fluorobenzyl) analogues of HIV drugs emivirine and GCA-186

[2] Esben R Sørensen, et al. Arch Pharm (Weinheim). Synthesis of 6-(3,5-dichlorobenzyl) derivatives as isosteric analogues of the HIV drug 6-(3,5-dimethylbenzyl)-1-(ethoxymethyl)-5-isopropyluracil (GCA-186)

[3] A L Hopkins, et al. J Med Chem. Design of MKC-442 (emivirine) analogues with improved activity against drug-resistant HIV mutants

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