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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 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|
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
Tamoxifen is a estrogen receptor partial agonist/antagonist.
GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ.
RaloxifeneHcl(LY156758 Hcl) is a second generation selective estrogen receptor antagonist.
Progesterone is an endogenous steroid hormone involved in the menstrual cycle, pregnancy, and embryogenesis of humans and other species. A potent agonist of the nuclear progesterone receptor (nPR) with Kd of 1 nM; An agonist of the membrane progesterone receptors(mPRs); An antagonist of the σ1 receptor.
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