GW1929

GW1929 화학적 특성, 용도, 생산

• 개요

  Peroxisome proliferator-activated receptor (PPAR) γ is a nuclear receptor that, when activated, regulates fatty acid storage and glucose metabolism. The best known class of PPARγ ligands are the thiazolidinediones, including troglitazone and rosiglitazone. GW 1929 is a non-thiazolidinedione activator of PPARγ that binds with a Ki value of 1.4 nM, with greater than 1,000-fold selectivity over other PPAR subtypes. It has anti-hyperglycemic and anti-hyperlipidemic activity when given orally in mouse and rat models of type 2 diabetes. Both in vitro and in vivo effects of GW 1929 on PPARγ greatly exceed those produced by troglitazone. In addition, GW 1929 has neuroprotective effects in global cerebral ischemic-reperfusion injury that are related to reduced inflammation and apoptotic DNA fragmentation.

• 용도

  GW1929 has been used as a peroxisome proliferator-activated receptor γ (PPARγ) ligand:
  Investigating its impact on the expression of plant homeodomain finger protein 16 (Phf16) and patatin-like phospholipase domain containing 3 (Pnpla3) in relation to adipogenesis.
  Examining its influence on complement component 3 (C3) gene expression in human hepatoma cells.
  Activating PPARγ in human breast cancer cells.

• 생물학적 활성

  Highly selective orally active peroxisome proliferator-activated receptor (PPAR) γ agonist (pEC 50 values are 8.05, < 4 and < 4 for human PPAR γ , PPAR α and PPAR δ receptors respectively). Decreases glucose, fatty acid and triglyceride levels following oral administration in vivo .

• 참고 문헌

  [1] heppner tj,bonev ad,eckman dm,gomez mf,petkov gv,nelson mt. novel ppargamma agonists gi 262570, gw 7845, gw 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries. pharmacology.2005 jan;73(1):15-22.
  [2] kaundal rk,sharma ss. ameliorative effects of gw1929, a nonthiazolidinedione pparγ agonist, on inflammation and apoptosis in focal cerebral ischemic-reperfusion injury. curr neurovasc res.2011 aug 1;8(3):236-45.
  [3] GW1929: a nonthiazolidinedione PPARγ agonist, ameliorates neurological damage in global cerebral ischemic-reperfusion injury through reduction in inflammation and DNA fragmentation DOI: 10.1016/j.bbr.2010.09.001

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