| 货号 | 10004888-25g |
| 描述 | Peroxisome proliferator-activated receptor γ (PPARγ) isoforms heterodimerize with retinoic X receptors to modulate gene expression related to adipocyte differentiation, fatty acid uptake and storage, and glucose metabolis.1 Natural agonists of PPARγ include fatty acids (e.g., linoleic acid and 15-deoxy-Δ12,14-prostaglandin J2), while thiazolidinediones (e.g., rosiglitazone and pioglitazone) are potent synthetic agonists.2,3 FMOC-L-leucine is a partial agonist of PPARγ.4,2 It activates PPARγ with a lower potency (Ki = 15 versus 0.035 µM) but a similar maximal efficacy compared to rosiglitazone.4 FMOC-L-leucine improves insulin resistance in normal, diet-induced glucose-intolerant and in diabetic db/db mice, yet has reduced adipogenic activity.4 As a result, it is classified as a selective PPARγ modulator (SPPARM), capable of producing insulin-sensitizing effects while minimizing side effects associated with full agonists.2 |
| 别名 | FMOC-Leu;NPC 15199;NSC 334290; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Heikkinen, S.,Auwerx, J., and Argmann, C.A. PPARγ in human and mouse physiology. Biochimica et Biophysica Acta 1771(8), 999-1013 (2007). 2.Villacorta, L.,Schopfer, F.J.,Zhang, J., et al. PPARγ and its ligands: Therapeutic implications in cardiovascular disease. Clinical Science 116, 205-218 (2009). 3.Zieleniak, A.,Wójcik, M., and Wozniak, L.A. Structure and physiological functions of the human peroxisome proliferator-activated receptor γ. Archivum Immunologiae et Therapiae Experimentalis 56, 331-345 (2008). 4.Rocchi, S.,Picard, F.,Vamecq, J., et al. A unique PPARγ ligand with potent insulin-sensitizing yet weak adipogenic activity. Molecular Cell 8, 737-747 (2001). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | 22 |
| 纯度 | ≥98% |
| 计算分子量 | 353.4 |
| 分子式 | C21H23NO4 |
| CAS号 | 35661-60-0 |
| 稳定性 | ≥ 2 years |
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