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Nomegestrol acetate

Cat. No. M8236
Nomegestrol acetate Structure
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Biological Activity

Nomegestrol acetate (NOMAc) is a potent, highly selective progestogen, a full agonist at the progesterone receptor, with no or minimal binding to other steroid receptors. It shows potent antigonadotropic activity mediated at the hypothalamic and pituitary level with strong antiestrogenic effects and a partial antiandrogenic effect. NOMAc is used in various formulations as a contraceptive.

Chemical Information
Molecular Weight 370.48
Formula C23H30O4
CAS Number 58652-20-3
Solubility (25°C) DMSO: ≥7 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] Hannat Akintomide, et al. Nomegestrol acetate/17-beta estradiol: a review of efficacy, safety, and patient acceptability

[2] Lino Del Pup, et al. Nomegestrol acetate/estradiol hormonal oral contraceptive and breast cancer risk

[3] Xiangyan Ruan, et al. The pharmacology of nomegestrol acetate

[4] Stefano Lello. Nomegestrol acetate: pharmacology, safety profile and therapeutic efficacy

[5] S Lello. Nomegestrol acetate: clinical pharmacology

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