DY131 appears to inhibit Smo signaling through a common binding site shared by previously reported Smo agonists and antagonists. Sox2-Cre:Errβ+/lox and Sox2-Cre:Errβlox/lox mice treated with the Errβ and Errγ agonist DY131 demonstrated increased corticotropin-releasing hormone (Crh) expression in the paraventricular nucleus of the hypothalamus, although corticosterone levels were not affected. Adrenal Cyp11b1 and Cyp11b2 mRNA were increased in pregnant WT mice treated with DY131. In this study,using RNA knockdown and transcriptional activation with DY131 (an ERRγ agonist), we clearly demonstrated that ERRγ promotes hormone production and cell fusion indicating that ERRγ is a key positive transcriptional factor involved in CT differentiation.
|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 100 mg/mL
Ethanol 10 mg/mL
Trophoblast syncytialisation necessitates mitochondrial function through estrogen-related receptor-γ activation.
Poidatz D, et al. Mol Hum Reprod. 2014 Nov 6. PMID: 25376642.
Estrogen-related receptor γ serves a role in blood pressure homeostasis during pregnancy.
Luo Y, et al. Mol Endocrinol. 2014 Jun;28(6):965-75. PMID: 24725083.
Estrogen-related receptor β deficiency alters body composition and response to restraint stress.
Byerly MS, et al. BMC Physiol. 2013 Sep 22;13:10. PMID: 24053666.
Selective identification of hedgehog pathway antagonists by direct analysis of smoothened ciliary translocation.
Wang Y, et al. ACS Chem Biol. 2012 Jun 15;7(6):1040-8. PMID: 22554036.
|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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