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Cyclosporin A-Derivative 1

Cat. No. M22059
Cyclosporin A-Derivative 1 Structure
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Biological Activity

Cyclosporin A-Derivative 1

Chemical Information
Molecular Weight 1364.5
Formula C65H118BF4N11O14
CAS Number 1487360-85-9
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] Emese Tth, et al. J Physiol. Novel mitochondrial transition pore inhibitor N-methyl-4-isoleucine cyclosporin is a new therapeutic option in acute pancreatitis

[2] Satoshi Sasamura, et al. J Antibiot (Tokyo). Bioconversion of FR901459, a novel derivative of cyclosporin A, by Lentzea sp. 7887

[3] Luca Azzolin, et al. PLoS One. Antamanide, a derivative of Amanita phalloides, is a novel inhibitor of the mitochondrial permeability transition pore

[4] Koichi Watashi. Curr Opin Investig Drugs. Alisporivir, a cyclosporin derivative that selectively inhibits cyclophilin, for the treatment of HCV infection

[5] Z R Lu, et al. Bioconjug Chem. Modification of cyclosporin A and conjugation of its derivative to HPMA copolymers

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