557366-M
罗格列酮
A thiazolidinedione compound that acts as an anti-diabetic agent and serves as a potent and selective agonist of peroxisome proliferator-activated receptor-γ (PPARγ) (Kd ~40 nM) in fat cells.
别名:
罗格列酮
SMILES string
S1C(C(=O)[N+H2]C1=O)Cc2ccc(cc2)OCC[N+H](C)c3ncccc3.[O-]C(=O)\C=C/C(=O)[O-]
InChI
1S/C18H19N3O3S.C4H4O4/c1-21(16-4-2-3-9-19-16)10-11-24-14-7-5-13(6-8-14)12-15-17(22)20-18(23)25-15;5-3(6)1-2-4(7)8/h2-9,15H,10-12H2,1H3,(H,20,22,23);1-2H,(H,5,6)(H,7,8)/b;2-1-
InChI key
SUFUKZSWUHZXAV-BTJKTKAUSA-N
assay
≥99% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
storage temp.
−20°C
Quality Level
General description
一种噻唑烷二酮类化合物，作为抗糖尿病药物，并作为脂肪细胞中过氧化物酶体增殖物激活受体-g（PPARg）（Kd~40 nM）的有效和选择性激动剂。在II型糖尿病的动物模型中显示减少脂肪酸摄取和改善脂质代谢和胰岛素抵抗。据报道可激活含a1和a2的AMPK复合物。与曲格列酮不同，它不会诱导 P4503A4 的活性。显着改善C3H10T1/2干细胞向脂肪细胞的分化。显示通过干扰雄激素与芳香化酶的结合阻止雌激素合成，但不影响芳香化酶mRNA或蛋白质表达。
Preparation Note
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多3个月。
Other Notes
Araki, T., et al. 2011.PPAR Res.2011, 926438.
Sozio, M. S., et al. 2011. Am. J. Physiol.Gastrointest.Liver Physiol.301, G739.
Gerstein, H., et al. 2006.Drug 368, 9541.
Mohanty, P., 2004.Journ.Clin. Endocrin. & Metab. 89(6), 2728-2735.
Fryer, L., et al. 2002.J Biol Chem 277, 25226.
Goldberg, R., et al. 1999.Drug. 57, 921.
Young, P., et al. 1998.Journ.Pharm. Exp.Ther. 284, 751.
Willson, T., et al. 1996.J. Med. Chem.39, 665; Lehmann, J., et al., 1995. JBC270, 12953.
Cantello, B., et al., 1994.Bioorg.Med. Chem. Lett.4, 1181.
Sozio, M. S., et al. 2011. Am. J. Physiol.Gastrointest.Liver Physiol.301, G739.
Gerstein, H., et al. 2006.Drug 368, 9541.
Mohanty, P., 2004.Journ.Clin. Endocrin. & Metab. 89(6), 2728-2735.
Fryer, L., et al. 2002.J Biol Chem 277, 25226.
Goldberg, R., et al. 1999.Drug. 57, 921.
Young, P., et al. 1998.Journ.Pharm. Exp.Ther. 284, 751.
Willson, T., et al. 1996.J. Med. Chem.39, 665; Lehmann, J., et al., 1995. JBC270, 12953.
Cantello, B., et al., 1994.Bioorg.Med. Chem. Lett.4, 1181.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
wgk
WGK 3
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