SR 16832 是一种双位点共价 PPARγ 抑制剂，作用于正构和变构位点 。
| Cas No. | 2088135-12-8 |
| Canonical SMILES | COC1=CC=C2C(C(NC(C3=CC([N+]([O-])=O)=CC=C3Cl)=O)=CC=N2)=C1 |
| 分子式 | C17H12ClN3O4 |
| 分子量 | 357.7 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SR 16832 is a dual-site covalent antagonist of peroxisome proliferator-activated receptor γ (PPARγ).1 It inhibits MRL20-induced allosteric activation of PPARγ in a reporter assay using HEK293T cells when used at a concentration of 5 μM. SR 16832 also reduces basal activity of PPARγ and inhibits binding of docosahexaenoic acid to PPARγ in a time-resolved FRET (TR-FRET) assay. References
1. Brust, R., Lin, H., Fuhrmann, J., et al. Modification of the orthosteric PPARγ covalent antagonist scaffold yields an improved dual-site allosteric inhibitor. ACS Chem. Biol. 12(4), 969-978 (2017). |
