Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
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Source | J Clin Pharmacol (2012). Figure 1. Norethindrone |
| Method | PK and Pharmacodynamic (PD) Assessments | |
| Cell Lines | ||
| Concentrations | 0.5 mg/kg | |
| Incubation Time | 1, 7, 14, 21, 22, 28, 35, 42, 49, 50, and 56 days | |
| Results | Mean steady-state Cmax, AUC, and Cmin and their 90% CIs of their GLSMRs fell within the no-effect limit boundary of 0.80 to 1.25. |
| Cell Experiment | |
|---|---|
| Cell lines | Human epithelial cervical cancer cells |
| Preparation method | Thereafter, the cells were incubated with serum-free, phenol-free DMEM for 2 hrs, before treatment with 100 nM DEX, MPA, P4 and NET-A for 1 hr. Cells were crosslinked for 10 min at 37°C with1% formaldehyde and the reaction was stopped with 0.1 mM glycine for 5 min, shaking at room temperature. |
| Concentrations | 100 nM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | Female Sprague-Dawley rats |
| Formulation | corn oil |
| Dosages | 3 μg/rat/day |
| Administration | oral |
| Molecular Weight | 298.42 |
| Formula | C20H26O2 |
| CAS Number | 68-22-4 |
| 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.
| Related Progesterone Receptor Products |
|---|
| 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. |
| Cridanimod
Cridanimod is a potent progesterone receptor (PR) activator mediated through induction of IFNα and IFNβ expression. Cridanimod is a small-molecule immunomodulator and interferon inducer. |
| Asoprisnil
Asoprisnil (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human. |
| Medroxyprogesterone
Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist. |
| Nestorone
Nestorone is a potent progesterone receptor agonist with no androgenic, estrogenic, or glucocorticoid-like activities. |
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