Gestodene is a progestogen hormonal contraceptive. Gestodene displays a high binding affinity to the progesterone receptor, and also binds strongly to adrogen and glucocorticoid receptors.
| Molecular Weight | 310.43 |
| Formula | C21H26O2 |
| CAS Number | 60282-87-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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.
[1] Marcos de Bastos, et al. Combined oral contraceptives: venous thrombosis
[3] H Kuhl, et al. Gestodene-containing contraceptives
[5] D Shoupe. New progestins--clinical experiences: gestodene
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| Nomegestrol
Nomegestrol is a potent and orally available progestin, acts as a selective full progesterone receptor agonist, with a Kd of 5.44 nM for rat uterine progesterone receptor, and has moderate antiandrogenic activity and strong antiestrogenic activity. |
| Allylestrenol
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| Cridanimod
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| Asoprisnil
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