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Antimalarial agent 12

Cat. No. M38782
Antimalarial agent 12 Structure
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Biological Activity

Antimalarial agent 12 is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines.

Chemical Information
Molecular Weight 505.79
Formula C26H18BrClN2O2
CAS Number 2715225-58-2
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] Bishnu Prasad Raiguru et al. Bioorg Chem. Recent developments in the synthesis of hybrid antimalarial drug discovery

[2] Anwei Hou et al. Chembiochem. Cladosporin, A Highly Potent Antimalaria Drug?

[3] Jorddy N Cruz et al. Comb Chem High Throughput Screen. Antimalarial Hemozoin Inhibitors (β-Hematin Formation Inhibition): Latest Updates

[4] Livia Neves Borgheti-Cardoso et al. Future Med Chem. Turning Plasmodium survival strategies against itself

[5] Duong Nhu et al. Bioorg Med Chem Lett. Antimalarial 3-arylamino-6-benzylamino-1,2,4,5-tetrazines

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