422175
L-165,041
A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPARδ and 730 nM for hPPARγ).
别名:
L-165,041, Compound P, L165041, 4-[3-(2-Propyl-3-hydroxy-4-acetyl)phenoxy]propyloxyphenoxy-acetic acid, PPAR Agonist VIII, PPARα Agonist III, PPARγ Agonist VII
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About This Item
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质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
1 M NaOH: 40 mg/mL
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
O(CCCOc2ccc(cc2)OCC(=O)O)c1c(c(c(cc1)C(=O)C)O)CCC
InChI
1S/C22H26O7/c1-3-5-19-20(11-10-18(15(2)23)22(19)26)28-13-4-12-27-16-6-8-17(9-7-16)29-14-21(24)25/h6-11,26H,3-5,12-14H2,1-2H3,(H,24,25)
InChI key
HBBVCKCCQCQCTJ-UHFFFAOYSA-N
一般描述
A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPAR δ and 730 nM for hPPARγ). Induces adipocyte differentiation in NIH-PPARδ cells at 500 nM. Also reported to raise total cholesterol in insulin-resistant db/db mice without altering glucose or triglyceride levels. Shown to increase uncoupling protein 3 (UCP3) gene expression in L6 myotubes. Also shown to inhibit cytokine-induced expression of vascular cell adhesion molecule-1 (VCAM-1) and the secretion of monocyte chemotactic protein-1 (MCP-1) in Eahy926 cells.
A cell-permeable phenoxyacetic acid derivative that acts as a potent and selective peroxisome proliferator activator receptor δ (PPARδ) agonist (Ki = 6 nM for hPPARδ and 730 nM for hPPARγ). Potently induces adipocyte differentiation in NIH-PPARδ cells at 500 nM and raises total cholesterol in insulin resistant db/db mice without altering glucose or triglycerides levels. Increases UCP3 (uncoupling protein 3) gene expression in L6 myotubes. Inhibits cytokine-induced expression of VCAM-1 (vascular cell adhesion molecule-1) and the secretion of MCP-1 (monocyte chemotactic protein-1) in EAhy926 cells.
生化/生理作用
Cell permeable: yes
Primary Target
Peroxisome proliferator activator receptor δ (PPAR@delta;)
Peroxisome proliferator activator receptor δ (PPAR@delta;)
Product does not compete with ATP.
Reversible: no
Target Ki: 6 nM for hPPARδ and 730 nM for hPPARγ
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
重悬
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Rival, Y., et al. 2002. Eur. J. Pharmacol.435, 143.
Castrillo, A., et al. 2001. J. Biol. Chem.276, 34082.
Hansen, J.B., et al. 2001. J. Biol. Chem.276, 3175.
Son, C., et al. 2001. Endocrinology142, 4189.
Wilkie, N., et al. 2001. J. Neurochem.78, 1135.
Leibowitz, M.D., et al. 2000. FEBS Lett.473, 333.
Berger, J., et al. 1999. J. Biol. Chem.274, 6718.
Lim, H., et al. 1999. Genes Dev.13, 1561.
Castrillo, A., et al. 2001. J. Biol. Chem.276, 34082.
Hansen, J.B., et al. 2001. J. Biol. Chem.276, 3175.
Son, C., et al. 2001. Endocrinology142, 4189.
Wilkie, N., et al. 2001. J. Neurochem.78, 1135.
Leibowitz, M.D., et al. 2000. FEBS Lett.473, 333.
Berger, J., et al. 1999. J. Biol. Chem.274, 6718.
Lim, H., et al. 1999. Genes Dev.13, 1561.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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