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213252-19-8
  • names:

    5-((2,4-Dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide

  • CAS号:

    213252-19-8

    MDL Number:
  • MF(分子式): C20H17F3N2O4S MW(分子量): 438.42
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
KRP297
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中文别名 KRP297
英文别名 KRP297; KRP-297; KRP 297; L 410198; L410198; MK-0767; MK-767.
CAS号 213252-19-8
SMILES O=C(NCC1=CC=C(C(F)(F)F)C=C1)C2=CC(CC(SC(N3)=O)C3=O)=CC=C2OC
Inchi InChI=1S/C20H17F3N2O4S/c1-29-15-7-4-12(9-16-18(27)25-19(28)30-16)8-14(15)17(26)24-10-11-2-5-13(6-3-11)20(21,22)23/h2-8,16H,9-10H2,1H3,(H,24,26)(H,25,27,28)
InchiKey NFFXEUUOMTXWCX-UHFFFAOYSA-N
分子式 Formula C20H17F3N2O4S
分子量 Molecular Weight 438.42
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 KRP297(CAS:213252-19-8):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionKRP297, also known as MK-0767 and MK-767, is a PPAR agonist potentially for the treatment of type 2 diabetes and dyslipidemia. When administered to ob/ob mice, KRP-297 (0.3 to 10 mg/kg) decreased plasma glucose and insulin levels and improved the impaired insulin-stimulated 2DG uptake in soleus muscle in a dose-dependent manner. KRP-297 treatment is useful to prevent the development of diabetic syndromes in addition to ameliorating the impaired glucose transport in skeletal muscle.
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[1]Xu XS, Yan KX, Song H, Lo MW. Quantitative determination of a novel dual PPAR alpha/gamma agonist using on-line turbulent flow extraction with liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Jan 5;814(1):29-36. PubMed PMID: 15675045.
[2]Miyachi H. [Design and synthesis of subtype- and species-selective peroxisome proliferator-activated receptor (PPAR) alpha ligands]. Yakugaku Zasshi. 2004 Nov;124(11):803-13. Review. Japanese. PubMed PMID: 15516807.
[3] Narce M, Poisson JP. Novel PPARgamma-dependent and independent effects for thiazolidinediones. Curr Opin Lipidol. 2003 Dec;14(6):651-2. PubMed PMID: 14624145.
[4] Calkin AC, Thomas MC, Cooper ME. MK-767. Kyorin/Banyu/Merck. Curr Opin Investig Drugs. 2003 Apr;4(4):444-8. Review. PubMed PMID: 12808885.
[5] Yajima K, Hirose H, Fujita H, Seto Y, Fujita H, Ukeda K, Miyashita K, Kawai T, Yamamoto Y, Ogawa T, Yamada T, Saruta T. Combination therapy with PPARgamma and PPARalpha agonists increases glucose-stimulated insulin secretion in db/db mice. Am J Physiol Endocrinol Metab. 2003 May;284(5):E966-71. Erratum in: Am J Physiol Endocrinol Metab. 2003 Oct;285(4):E926. PubMed PMID: 12676649.
6: Yamanouchi T. [KRP-297, MCC-555]. Nihon Rinsho. 2001 Nov;59(11):2200-6. Review. Japanese. PubMed PMID: 11712408.7: Murakami K, Ide T, Nakazawa T, Okazaki T, Mochizuki T, Kadowaki T. Fatty-acyl-CoA thioesters inhibit recruitment of steroid receptor co-activator 1 to alpha and gamma isoforms of peroxisome-proliferator-activated receptors by competing with agonists. Biochem J. 2001 Jan 15;353(Pt 2):231-8. PubMed PMID: 11139385; PubMed Central PMCID: PMC1221563.8: Chaput E, Saladin R, Silvestre M, Edgar AD. Fenofibrate and rosiglitazone lower serum triglycerides with opposing effects on body weight. Biochem Biophys Res Commun. 2000 May 10;271(2):445-50. PubMed PMID: 10799317.9: Ide T, Nakazawa T, Mochizuki T, Murakami K. Tissue-specific actions of antidiabetic thiazolidinediones on the reduced fatty acid oxidation in skeletal muscle and liver of Zucker diabetic fatty rats. Metabolism. 2000 Apr;49(4):521-5. PubMed PMID: 10778879.10: Murakami K, Tsunoda M, Ide T, Ohashi M, Mochizuki T. Amelioration by KRP-297, a new thiazolidinedione, of impaired glucose uptake in skeletal muscle from obese insulin-resistant animals. Metabolism. 1999 Nov;48(11):1450-4. PubMed PMID: 10582556.1
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