Name: MD001
Rating: 5 (10 reviews)

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HIT ID:HIT214320789
Cas No:2254605-76-8
常用名:MD001
IUPAC:5,7-dihydroxy-8-methyl-4-phenyl-3-[(2E)-3-phenylprop-2-enoyl]-2H-chromen-2-one
IUPAC:5,7-dihydroxy-8-methyl-4-phenyl-3-[(2E)-3-phenylprop-2-enoyl]-2H-chromen-2-one
InChI key:RTYVORPNMMHKDM-OUKQBFOZSA-N

分子式:C25H18O5
分子量:398.414
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:Cc1c(O)cc(O)c2c(-c3ccccc3)c(C(=O)\C=C\c3ccccc3)c(=O)oc12
SMILES:Cc1c(O)cc(O)c2c(-c3ccccc3)c(C(=O)\C=C\c3ccccc3)c(=O)oc12

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.

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