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Norgestimate

Cat. No. M8305
Norgestimate Structure
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Biological Activity

Norgestimate is a synthetic progestin used in combination with estrogens as a contraceptive.

Chemical Information
Molecular Weight 369.5
Formula C23H31NO3
CAS Number 35189-28-7
Solubility (25°C) DMSO: 5 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] Giovanni Grandi, et al. The paradigm of norgestimate: a third-generation testosterone-derivative progestin with a peripheral anti-androgenic activity and the lowest risk of venous thromboembolism

[2] S L Corson. Norgestimate

[3] J L McGuire, et al. Pharmacologic and pharmacokinetic characteristics of norgestimate and its metabolites

[4] J Bringer. Norgestimate: a clinical overview of a new progestin

[5] A Phillips, et al. Preclinical evaluation of norgestimate, a progestin with minimal androgenic activity

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