DPN increased GluR2 expression in the other lamina of the CA1.DPN acts as an agonist on both ER subtypes, but has a 70-fold higher relative binding affinity and 170-fold higher relative potency in transcription assays with ERbeta than with ERalpha. DPN displayed subtype-selective agonism, being ca. 30-fold more potent through ERbeta.Both PPT and DPN can acutely relax isolated mesenteric arteries with the relative potency of PPT>17beta-oestrogen>DPN.
|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.
Estrogen receptor alpha and beta specific agonists regulate expression of synaptic proteins in rat hippocampus.
Waters EM, et al. Brain Res. 2009 Sep 22;1290:1-11. PMID: 19596275.
Activities of estrogen receptor alpha- and beta-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression.
Harrington WR, et al. Mol Cell Endocrinol. 2003 Aug 29;206(1-2):13-22. PMID: 12943986.
Acute effects of oestrogen receptor subtype-specific agonists on vascular contractility.
Montgomery S, et al. Br J Pharmacol. 2003 Aug;139(7):1249-53. PMID: 12890703.
Estrogen receptor-beta potency-selective ligands: structure-activity relationship studies of diarylpropionitriles and their acetylene and polar analogues.
Meyers MJ, et al. J Med Chem. 2001 Nov 22;44(24):4230-51. PMID: 11708925.
|Related Estrogen Receptor Products|
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.
4-Hydroxytamoxifen is a selective estrogen receptor modulator.
Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.
|Endoxifen E-isomer hydrochloride
Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).
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