Norethindrone is a synthetic progestin, which mimic the actions of the endogenous ovarian hormone progesterone.
|Source||J Clin Pharmacol (2012). Figure 1. Norethindrone|
|Method||PK and Pharmacodynamic (PD) Assessments|
|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 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.|
|Incubation time||1 h|
|Animal models||Female Sprague-Dawley rats|
|Solubility (25°C)||DMSO 50 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Africander DJ, et al. J Steroid Biochem Mol Biol. A comparative study of the androgenic properties of progesterone and the progestins, medroxyprogesterone acetate (MPA) and norethisterone acetate (NET-A).
 Govender Y, et al. PLoS One. The injectable-only contraceptive medroxyprogesterone acetate, unlike norethisterone acetate and progesterone, regulates inflammatory genes in endocervical cells via the glucocorticoid receptor.
|Related Progesterone Receptor Products|
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 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 (J867), a selective progesterone receptor modulator, exhibits mixed progesterone agonist and antagonist effects on various progesterone targeted tissues in animal and human.
Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
Nestorone is a potent progesterone receptor agonist with no androgenic, estrogenic, or glucocorticoid-like activities.
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