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.
| Molecular Weight | 311.38 |
| Formula | C18H21N3O2 |
| CAS Number | 95167-41-2 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Related Estrogen Receptor Products |
|---|
| hFSH-β-(33-53) TFA
hFSH-β-(33-53) TFA, a thiol-containing peptide which corresponds to a second FSH receptor-binding domain, is a FSHR (follicle-stimulating hormone receptor) antagonist. hFSH-β-(33-53) TFA inhibits binding of FSH to receptor and is a partial agonist of estradiol synthesis in Sertoli cells. |
| Yp537
Yp537 is an estrogen receptor (ER) inhibitor that blocks dimerization of the human estrogen receptor. |
| Palazestrant
Palazestrant is a novel, orally active, estrogen receptor antagonist and selective estrogen receptor degrader. It can be used in studies related to ER+/HER2+ breast cancer. |
| Acolbifene hydrochloride
Acolbifene hydrochloride is an active metabolite of EM800 and an orally available, selective estrogen receptor modulator (SERM) that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity, has significant anti-estrogenic effects on the mammary gland and uterus, and has anticancer activity. possesses anticancer activity. |
| Acolbifene
Acolbifene is an active metabolite of EM800 and an orally active pure anti-estrogen and selective estrogen receptor (ER) antagonist that inhibits estradiol-induced ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM) transcriptional activity and has anticancer activity. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
