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Chemical Compound Review

Galida     (2S)-2-ethoxy-3-[4-[2-(4...

Synonyms: Tesaglitazar, CHEMBL282686, AZ-242, AG-K-12760, ANW-48037, ...
 
 
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Disease relevance of Galida

 

Psychiatry related information on Galida

  • A second group received the same HC supplement along with tesaglitazar (T) 0.5 micromol/kg diet (T group) [3].
 

High impact information on Galida

  • Tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist, dose-dependently improves the metabolic abnormalities associated with insulin resistance in a non-diabetic population [4].
  • RESULTS: A 1.0-mg dose of tesaglitazar reduced fasting triglycerides (the primary endpoint) by 37% (95% CI: -43% to -30%; p<0.0001), non-HDL-cholesterol by 15% (95% CI: -20% to -10%; p<0.0001) and NEFA by 40% (95% CI: -51% to -27%; p<0.0001), and increased HDL-cholesterol by 16% (95% CI: 8 to -24%; p<0.0001) [4].
  • Peroxisome proliferator-activated receptor (PPAR) activation induces tissue-specific effects on fatty acid uptake and metabolism in vivo--a study using the novel PPARalpha/gamma agonist tesaglitazar [5].
  • To test this hypothesis directly, we examined the effect of the novel PPARalpha/gamma agonist tesaglitazar on whole-body insulin sensitivity and NEFA clearance into epididymal white adipose tissue (WAT), red gastrocnemius muscle, and liver in rats with dietary-induced insulin resistance [5].
  • In vitro, in reporter gene assays, AZ 242 activated human PPARalpha and PPARgamma with EC(50) in the micro molar range [1].
 

Biological context of Galida

 

Anatomical context of Galida

  • We present pharmacodynamic effects of AZ 242, a novel peroxisome proliferator activated receptor (PPAR)alpha/gamma agonist [1].
  • In addition, tesaglitazar reduced inflammatory markers, including plasma SAA levels, the number of adhering monocytes, and nuclear factor kappaB-activity in the vessel wall [3].
 

Associations of Galida with other chemical compounds

 

Gene context of Galida

  • In anesthetized, 5-h fasted, obese Zucker rats, tesaglitazar reduced hepatic TG secretion by 47%, increased plasma TG clearance by 490%, and reduced very low-density lipoprotein (VLDL) apolipoprotein CIII content by 86%, compared with obese controls [9].
 

Analytical, diagnostic and therapeutic context of Galida

References

  1. AZ 242, a novel PPARalpha/gamma agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats. Ljung, B., Bamberg, K., Dahllöf, B., Kjellstedt, A., Oakes, N.D., Ostling, J., Svensson, L., Camejo, G. J. Lipid Res. (2002) [Pubmed]
  2. Tesaglitazar. Kamber, N., Davis, T.M. IDrugs : the investigational drugs journal. (2005) [Pubmed]
  3. Dual PPARalpha/gamma agonist tesaglitazar reduces atherosclerosis in insulin-resistant and hypercholesterolemic ApoE*3Leiden mice. Zadelaar, A.S., Boesten, L.S., Jukema, J.W., van Vlijmen, B.J., Kooistra, T., Emeis, J.J., Lundholm, E., Camejo, G., Havekes, L.M. Arterioscler. Thromb. Vasc. Biol. (2006) [Pubmed]
  4. Tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist, dose-dependently improves the metabolic abnormalities associated with insulin resistance in a non-diabetic population. Fagerberg, B., Edwards, S., Halmos, T., Lopatynski, J., Schuster, H., Stender, S., Stoa-Birketvedt, G., Tonstad, S., Halldórsdóttir, S., Gause-Nilsson, I. Diabetologia (2005) [Pubmed]
  5. Peroxisome proliferator-activated receptor (PPAR) activation induces tissue-specific effects on fatty acid uptake and metabolism in vivo--a study using the novel PPARalpha/gamma agonist tesaglitazar. Hegarty, B.D., Furler, S.M., Oakes, N.D., Kraegen, E.W., Cooney, G.J. Endocrinology (2004) [Pubmed]
  6. Food does not affect the pharmacokinetics of tesaglitazar, a novel dual peroxisome proliferator-activated receptor alpha/gamma agonist. Samuelsson, S., Johansson, S., Halldórsdóttir, S., Stenhoff, H., Ohman, K.P. Journal of clinical pharmacology. (2006) [Pubmed]
  7. Pharmacokinetics and metabolism of tesaglitazar, a novel dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist, after a single oral and intravenous dose in humans. Ericsson, H., Hamrén, B., Bergstrand, S., Elebring, M., Fryklund, L., Heijer, M., Ohman, K.P. Drug Metab. Dispos. (2004) [Pubmed]
  8. Effect of tesaglitazar, a dual PPAR alpha/gamma agonist, on glucose and lipid abnormalities in patients with type 2 diabetes: a 12-week dose-ranging trial. Goldstein, B.J., Rosenstock, J., Anzalone, D., Tou, C., Ohman, K.P. Current medical research and opinion (2006) [Pubmed]
  9. Tesaglitazar, a dual PPAR{alpha}/{gamma} agonist, ameliorates glucose and lipid intolerance in obese Zucker rats. Oakes, N.D., Thalén, P., Hultstrand, T., Jacinto, S., Camejo, G., Wallin, B., Ljung, B. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2005) [Pubmed]
  10. Tesaglitazar: A promising approach in type 2 diabetes. Cox, S.L. Drugs of today (Barcelona, Spain : 1998) (2006) [Pubmed]
 
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