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|
|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.
|Solubility||DMSO 50 mg/mL|
 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.
SPH3127 is an oral direct renin inhibitor (DRI) that is being developed for hypertension. The renin-angiotensin-aldosterone system is responsible for the regulation of blood pressure.
SAfit2 is a potent inhibitor of FK506-binding protein 51 (FKBP51) with a Ki value of 6 nM. SAfit2 has been used as a potential agent in the study of major depression, obesity, and chronic pain.
“lipid 10a” (Arcturus tunable lipid for RNA drug delivery).
BAY 1214784 is a potent, selective and orally active antagonist of the human gonadotropin-releasing hormone receptor (hGnRH-R).BAY 1214784 has the potential to be studied in uterine fibroids.
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