| CAS NO: | 1415252-61-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 558.7 |
| Cas No. | 1415252-61-7 |
| Formula | C37H38N2O3 |
| Solubility | ≤5mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| Chemical Name | 4'-[[5-[[[(1S)-1-[4-(1,1-dimethylethyl)phenyl]ethyl]amino]carbonyl]-2,3-dimethyl-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid |
| Canonical SMILES | CC(N1CC2=CC=C(C3=CC=CC=C3C(O)=O)C=C2)=C(C)C4=C1C=CC(C(N[C@@H](C)C5=CC=C(C(C)(C)C)C=C5)=O)=C4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: 30 nM
SR 2595 is an inverse agonist of PPARγ.
The nuclear receptor peroxisome proliferator-activated receptor gamma (PPARγ) is the key regulator of adipogenesis and the pharmacological target of the thiazolidinedione class of insulin sensitizers. Activation of PPARγ by thiazolidinediones can promote adipogenesis at the expense of osteoblast formation.
In vitro: SR 2595 was identified as an inverse agonist of PPARγ that repressed both transactivation and expression of the adipogenic marker fatty acid-binding protein 4 in differentiating murine preadipocytes. Moreover, the repression of PPARγ with SR 2595 promoted osteogenesis in cultured human mesenchymal stem cells (MSCs), as demonstrated by calcium phosphatase deposition. In addition, SR 2595 could also increase the expression of bone morphogenetic proteins BMP2 and BMP6 in MSCs [1].
In vivo: To determine whether pharmacological PPARg repression would impair insulin sensitivity, SR2595 was administered chronically to lean C57BL/6J mice. The PK properties of SR2595 were sufficient to support once daily oral dosing at 20 mg/kg. Lean C57BL/6J mice treated with SR2595 showed no significant change in insulin sensitivity as measured by insulin tolerance test, nor fasting insulin levels. In addition, no change in food consumption or body weight was observed during the treatment period [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Marciano, D. P.,Kuruvilla, D.S.,Boregowda, S.V., et al. Pharmacological repression of PPARγ promotes osteogenesis. Nature Communications 6, 1-7 (2015).
m.cnreagent.com