| Description | CD2665 is an orally active antagonist of retinoic acid receptor (RAR). For RARγ and RARβ, the Kis are 110 nM and 306 nM. |
| In vitro | 在3T3细胞中,CD2665(100 nM)抵消了ATRA、CD271(adapalene,一种RAR-β,γ激动剂)和CD2043(RAR-α,β,γ全激动剂)的抗增殖效应,使细胞数量和百分比LFCS恢复到对照水平[1]。 |
| In vivo | 在经过10个月乙醇摄入的小鼠中,CD2665 (0.6 mg/kg; s.c.) 降低了脑部RARβ mRNA水平(相对对照组下降50%),而RXR β/γ mRNA水平未见明显变化[2]。 |
| Target activity | RARβ:306 nM(ki), RARγ:(ki)110 nM |
| molecular weight | 486.6 |
| Molecular formula | C31H34O5 |
| CAS | 170355-78-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 22.5mg/mL (46.2mM) |
| References | 1. Kim MJ, et al. The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53. 2. Koyama E, et al.Premature Growth Plate Closure Caused by a Hedgehog Cancer Drug Is Preventable by Co-Administration of a Retinoid Antagonist in Mice. J Bone Miner Res. 2021 Jul;36(7):1387-1402. 3. Alfos S, Boucheron C, et al. A retinoic acid receptor antagonist suppresses brain retinoic acid receptor overexpression and reverses a working memory deficit induced by chronic ethanol consumption in mice. Alcohol Clin Exp Res. 2001 Oct;25(10):1506-14. |