| Description | ER-50891 is a potent retinoic acid receptor alpha (RARα) antagonist. er-50891 reduces the inhibitory effect of allosteric retinoic acid and restores osteoblast differentiation induced by bone morphogenetic protein 2. |
| In vitro | ER-50891 significantly antagonized the inhibition of ATRA and enhanced the total cell metabolic activity and proliferation of preosteoblasts. Dose-dependent assays show ER-50891 could also rescue ATRA inhibited OCN expression and mineralization with or without the induction of BMP. ER-50891 also suppressed the ALP activity that was synergistically enhanced by BMP and ATRA. Neither ATRA, nor ER-50891 or their combination significantly affected the level of BMP-induced phosphorylated Smad1/5. The antagonist of RARα, ER-50891 could significantly attenuate ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis.[3] |
| molecular weight | 432.51 |
| Molecular formula | C29H24N2O2 |
| CAS | 187400-85-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 10 mg/mL (23.12 mM), Sonication is recommended. |
| References | 1. Batran RZ, et al. New quinolone derivatives as neuropeptide S receptor antagonists: Design, synthesis, homology modeling, dynamic simulations and modulation of Gq/Gs signaling pathways. Bioorg Chem. 2021;111:104817. 2. Kyzer JL, et al. Investigation of selective retinoic acid receptor alpha antagonist ER-50891 and related analogs for male contraception [published online ahead of print, 2023 May 8]. Arch Pharm (Weinheim). 2023;e2300031. 3. Wang S, et al. The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation. Drug Des Devel Ther. 2020;14:297-308. 4. Sun W, et al. All-trans retinoic acid and human salivary histatin-1 promote the spreading and osteogenic activities of pre-osteoblasts in vitro. FEBS Open Bio. 2020;10(3):396-406. |