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Quantification of a Novel PPAR${gamma}$ Partial Agonist (S)-2-Ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry
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  • Quantification of a Novel PPAR${gamma}$ Partial Agonist (S)-2-Ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry
  • Quantification of a Novel PPAR${gamma}$ Partial Agonist (S)-2-Ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) in Rat Plasma Using Liquid Chromatography-Tandem Mass Spectrometry
저자명
Chae. Hye-Won,Jung. Hae-Hum,Kim. Eun-Jung,Shim. Hyun-Joo,Lim. Joong-In,Ji. Hye-Young,Lee. Hye-Suk
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2010년|33권 9호|pp.1389-1394 (6 pages)
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대한약학회
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

(S)-2-ethoxy-3-(4-{3-methyl-5-[4-(3-methyl-isoxazol-5-yl)-phenyl]thiophen-2-ylmethoxy}-phenyl)-propionic acid (PAM-1616) is a novel peroxisome proliferators-activated receptor ${gamma}$ (PPAR${gamma}$) partial agonist with excellent antihyperglycemic activity. It is a promising new drug candidate for the treatment of type-2 diabetes with reduced possibility of edema in vitro/in vivo. In order to evaluate the pharmacokinetics of PAM-1616, a reliable, selective and sensitive high-performance liquid chromatography/electrospray ionization tandem mass spectrometry was developed for the quantification of PAM-1616 in rat plasma. The analytes were extracted from rat plasma with ethyl acetate, separated on an Atlantis dC18 column with a mobile phase of 75% acetonitrile in 10 mM ammonium formate (pH 4.5), and detected by tandem mass spectrometry in the selective reaction monitoring mode. The calibration curve was linear ($r^2$ = 0.999) over the concentration range of 0.05-20.0 ${mu}g/mL$ and the lower limit of quantification was 0.05 ${mu}g/mL$. The coefficient of variation and relative error at four QC levels were 1.8% to 14.3% and -10.0% to 6.5%, respectively. The present method was successfully applied to the pharmacokinetic study of PAM-1616 after intravenous administration of PAM-1616 potassium at a dose of 1 mg/kg in rats.