PPT prevents ovariectomy-induced weight gain and loss of bone mineral density.PPT induces gene expression in the hypothalamus following systemic administration in vivo.In a short-term (4 d) uterotrophic assay, PPT was found to be as efficacious as 17alpha-ethinyl-17beta-estradiol in stimulating uterine weight gain and up-regulating complement 3 gene expression. In a 6-wk chronic model, PPT completely prevented the ovariectomy-induced body weight increase and loss of bone mineral density. It also increased uterine weight and markedly reduced plasma cholesterol levels in these mature animals. PPT was also effective in the brain. It increased progesterone receptor mRNA in the arcuate and ventromedial nuclei of the hypothalamus and prevented experimentally induced hot flushes.
|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.
 Harris HA, et al. Endocrinology. Characterization of the biological roles of the estrogen receptors, ERalpha and ERbeta, in estrogen target tissues in vivo through the use of an ERalpha-selective ligand.
 Kraichely DM, et al. Endocrinology. Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-alpha and estrogen receptor-beta: correlations with biological character and distinct differences among SRC coactivator family members.
|Related Estrogen Receptor Products|
Quinestrol is a synthetic estrogen that has the potential to be used in breast and prostate cancer related research.
Giredestrant (GDC-9545) is a potential "best-in-class" selective estrogen receptor inhibitor (SERD). Giredestrant can competitively bind with Estradiol in the ER ligand binding domain and induce conformational changes. Giredestrant has antitumor activity.
Zuclomiphene citrate is a cis isomer of clomiphene citrate. Zuclomiphene citrate has an anti-estrogen effect and inhibits the secretion of luteinizing hormone (LH) more than trans isomers. Zuclomiphene citrate is also an oral active cholesterol lowering agent.
27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.
SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.