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Cyclosporine

Cat. No. M20393
Cyclosporine Structure
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Biological Activity

Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.

Chemical Information
Molecular Weight 1202.61
Formula C62H111N11O12
CAS Number 79217-60-0
Solubility (25°C) DMSO 100 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] D Colombo, et al. J Biol Regul Homeost Agents. Cyclosporine in transplantation - a history of converging timelines

[2] C Paul, et al. Ann Dermatol Venereol. [Cyclosporine]

[3] J R Jeffery. Clin Biochem. Cyclosporine analogues

[4] J M Mazer. Rev Prat. [Cyclosporine and psoriasis]

[5] G Russell, et al. Semin Arthritis Rheum. Mechanisms of action of cyclosporine and effects on connective tissues

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