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Chemical Compound Review

Farglitazar     (2S)-3-[4-[2-(5-methyl-2- phenyl-1,3-oxazol...

Synonyms: CHEMBL107367, SureCN501024, KBioGR_002347, KBioSS_002350, CHEBI:40089, ...
 
 
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Disease relevance of GI-262570

  • Treatment of the 4-week HFD rats with a PPARgamma agonist GI262570 ameliorated the diet-induced hyperinsulinemia and dyslipidemia, and effectively restored muscle adiponectin (all p < 0.05) [1].
  • CONCLUSIONS: This study demonstrated that (a) PPARgamma agonists improved insulin sensitivity and ameliorated dyslipidemia in HF fed rats and ZDF rats, which were correlated with serum adiponectin; (b) Serum adiponectin was positively correlated with adipose FABP3 mRNA in GI262570-treated rats [2].
 

High impact information on GI-262570

  • On the contrary, the rebound effect after amiloride treatment potentiated GI262570-induced plasma volume expansion [3].
  • Regional hemodynamic effects of the N-(2-benzoylphenyl)-L-tyrosine peroxisome proliferator-activated receptor-gamma ligand, GI 262570 [(S)-2-(2-benzoylphenylamino)-3-[4-[2-(5-methyl-2-phenyl-2-oxazol-4-yl)ethoxy]phenyl]propionic acid], in conscious rats [4].
  • Administration of GI 262570 twice daily for 4 days caused a slowly developing, modest fall in mean arterial blood pressure, associated with a progressive, hyperemic hindquarters vasodilatation, but with no consistent changes in renal or mesenteric hemodynamics [4].
  • In 3T3-L1 adipocytes, GI262570 did not affect insulin-stimulated VEGF secretion [5].
  • Using Ba2+ (10 mmol/l) as the charge carrier through VDCC, the half-inhibition constants (IC50) for GI 262570, GW 7845, GW 1929, and pioglitazone were 2.0 +/- 0.5, 3.0 +/- 0.5, 5.0 +/- 0.7, and 10.0 +/- 0.8 mumol/l, respectively [6].
 

Biological context of GI-262570

 

Associations of GI-262570 with other chemical compounds

  • For arterial diameter measurements the IC50 values for GI 262570, GW 7845, GW 1929, and pioglitazone were 2.4, 4.1, 6.3, and 13.9 mumol/l, respectively [6].
 

Analytical, diagnostic and therapeutic context of GI-262570

  • Effects of a PPARgamma agonist, GI262570, on renal filtration fraction and nitric oxide level in conscious rats [7].

References

  1. Changes of skeletal muscle adiponectin content in diet-induced insulin resistant rats. Yang, B., Chen, L., Qian, Y., Triantafillou, J.A., McNulty, J.A., Carrick, K., Clifton, L.G., Han, B., Geske, R., Strum, J., Brown, K.K., Stimpson, S.A., Pahel, G. Biochem. Biophys. Res. Commun. (2006) [Pubmed]
  2. Serum adiponectin as a biomarker for in vivo PPARgamma activation and PPARgamma agonist-induced efficacy on insulin sensitization/lipid lowering in rats. Yang, B., Brown, K.K., Chen, L., Carrick, K.M., Clifton, L.G., McNulty, J.A., Winegar, D.A., Strum, J.C., Stimpson, S.A., Pahel, G.L. BMC Pharmacol. (2004) [Pubmed]
  3. GI262570, a peroxisome proliferator-activated receptor {gamma} agonist, changes electrolytes and water reabsorption from the distal nephron in rats. Chen, L., Yang, B., McNulty, J.A., Clifton, L.G., Binz, J.G., Grimes, A.M., Strum, J.C., Harrington, W.W., Chen, Z., Balon, T.W., Stimpson, S.A., Brown, K.K. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  4. Regional hemodynamic effects of the N-(2-benzoylphenyl)-L-tyrosine peroxisome proliferator-activated receptor-gamma ligand, GI 262570 [(S)-2-(2-benzoylphenylamino)-3-[4-[2-(5-methyl-2-phenyl-2-oxazol-4-yl)ethoxy]phenyl]propionic acid], in conscious rats. Gardiner, S.M., Nunez, D.J., Baer, P.G., Brown, K.K., Bennett, T. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  5. PPARgamma agonists diminish serum VEGF elevation in diet-induced insulin resistant SD rats and ZDF rats. Yang, B., Lin, P., Carrick, K.M., McNulty, J.A., Clifton, L.G., Winegar, D.A., Strum, J.C., Stimpson, S.A., Pahel, G.L. Biochem. Biophys. Res. Commun. (2005) [Pubmed]
  6. Novel PPARgamma agonists GI 262570, GW 7845, GW 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries. Heppner, T.J., Bonev, A.D., Eckman, D.M., Gomez, M.F., Petkov, G.V., Nelson, M.T. Pharmacology (2005) [Pubmed]
  7. Effects of a PPARgamma agonist, GI262570, on renal filtration fraction and nitric oxide level in conscious rats. Yang, B., Clifton, L.G., McNulty, J.A., Chen, L., Brown, K.K., Baer, P.G. J. Cardiovasc. Pharmacol. (2003) [Pubmed]
 
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