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LY518674 is a potent and selective PPAR-alpha antagonist with EC50 of 42 nM for human PPARα. LY518674 upregulates both ApoA-I production and catabolism in human subjects with the metabolic syndrome. LY518674 produced a dose-dependent increase in serum HDL-c, resulting in 208 +/- 15% elevation at optimum dose. In cultured hepatocytes, LY518674 produced 50% higher apoA-1 secretion, which was associated with increase in radiolabeled methionine incorporation in apoA-1.
| Molecular Weight | 409.48 |
| Formula | C23H27N3O4 |
| CAS Number | 425671-29-0 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PPAR Products |
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GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a Ki of 160 nM. |
| SR10221
SR10221, a noncovalent inverse agonist of PPARγ, represses downstream PPARγ target genes leading to growth inhibition in bladder cancer cell lines. |
| Amorfrutin B
Amorfrutin B is a highly potent natural peroxisome proliferation-activated receptor γ (PPARγ) agonist with oral activity with Ki values of 19 nM and EC50 values of 73 nM, respectively. |
| Netoglitazone
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| DSO-5a
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