| Description | LY2955303 is an effective and selective antagonist of retinoic acid receptor gamma (RARγ, Ki = 1.09 nM). |
| In vitro | RARγ的功能性Ki值为7.1±4.9 nM。LY2955303对RARα, RARβ和RARγ的结合Ki值分别为>1700, >2980和1.09 nM[1]。 |
| In vivo | 单次口服LY2955303在大鼠体内展示了随剂量变化的效应，不同的负重减少显示出药效学的反应，其中ED50为0.72 mg/kg[1]。 |
| Target activity | RARγ:1.09 nM(ki) |
| molecular weight | 578.74 |
| Molecular formula | C36H42N4O3 |
| CAS | 1433497-19-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 25 mg/mL (43.20 mM), Sonication and heating are recommended. |
| References | 1. Hughes NE, et al. Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3274-3277. |