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145739-56-6
  • Tetomilast (OPC6535)

  • names:

    6-[2-(3,4-diethoxyphenyl)-1,3-thiazol-4-yl]pyridine-2-carboxylic acid

  • CAS号:

    145739-56-6

    MDL Number:
  • MF(分子式): C19H18N2O4S MW(分子量): 370.42
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Tetomilast (OPC6535)
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中文别名 6-[2-(3,4-diethoxyphenyl)-1,3-thiazol-4-yl]pyridine-2-carboxylic acid
英文别名 OPC6535; OPC-6535; OPC 6535; Tetomilast
CAS号 145739-56-6
SMILES O=C(C1=NC(C2=CSC(C3=CC=C(OCC)C(OCC)=C3)=N2)=CC=C1)O
Inchi InChI=1S/C19H18N2O4S/c1-3-24-16-9-8-12(10-17(16)25-4-2)18-21-15(11-26-18)13-6-5-7-14(20-13)19(22)23/h5-11H,3-4H2,1-2H3,(H,22,23)
InchiKey XDBHURGONHZNJF-UHFFFAOYSA-N
分子式 Formula C19H18N2O4S
分子量 Molecular Weight 370.42
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 Tetomilast (OPC6535)(CAS:145739-56-6):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。
IntroductionTetomilast, also known as OPC6535, is a novel thiazole phosphodiesterase-4 (PDE-4) inhibitor, which may prove useful in both the treatment of inflammatory bowel disease (IBD) and chronic obstructive pulmonary disease (COPD). Tetomilast attenuates elastase-induced pulmonary emphysema through inhibition of oxidative stress in rabbits. Tetomilast suppressed production of proinflammatory cytokines from human monocytes and ameliorated chronic colitis in IL-10-deficient mice.
Application1
Application2
Application3
警示图
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危险性警示
安全声明
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备注
[1]Mulhall AM, Droege CA, Ernst NE, Panos RJ, Zafar MA. Phosphodiesterase 4 inhibitors for the treatment of chronic obstructive pulmonary disease: a review of current and developing drugs. Expert Opin Investig Drugs. 2015 Dec;24(12):1597-61[1]doi: 10.1517/13543784.2015.1094054. Epub 2015 Sep 30. PubMed PMID: 26419847.
[2]Song SD, Tang HF. [Progress in PDE4 targeted therapy for inflammatory diseases]. Zhejiang Da Xue Xue Bao Yi Xue Ban. 2014 May;43(3):353-8. Review. Chinese. PubMed PMID: 24998661.
[3] Bickston SJ, Snider KR, Kappus MR. Tetomilast: new promise for phosphodiesterase-4 inhibitors? Expert Opin Investig Drugs. 2012 Dec;21(12):1845-9. doi: 10.1517/13543784.2012.732065. Epub 2012 Oct 8. Review. PubMed PMID: 23043390.
[4] Baila B, Ohno Y, Nagamoto H, Kotosai K, Yabuuchi Y, Funaguchi N, Ito F, Endo J, Mori H, Takemura G, Fujiwara T, Fujiwara H, Minatoguchi S. Tetomilast attenuates elastase-induced pulmonary emphysema through inhibition of oxidative stress in rabbits. Biol Pharm Bull. 2012;35(4):494-502. PubMed PMID: 22466552.
[5] Salari P, Abdollahi M. Phosphodiesterase inhibitors in inflammatory bowel disease. Expert Opin Investig Drugs. 2012 Mar;21(3):261-4. doi: 10.1517/13543784.2012.658915. Epub 2012 Feb 6. PubMed PMID: 22303952.
6: Salari-Sharif P, Abdollahi M. Phosphodiesterase 4 inhibitors in inflammatory bowel disease: a comprehensive review. Curr Pharm Des. 2010;16(33):3661-7. Review. PubMed PMID: 21128899.7: Giembycz MA. Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking? Br J Pharmacol. 2008 Oct;155(3):288-90. doi: 10.1038/bjp.2008.297. Epub 2008 Jul 28. PubMed PMID: 18660832; PubMed Central PMCID: PMC2567889.8: Ichikawa H, Okamoto S, Kamada N, Nagamoto H, Kitazume MT, Kobayashi T, Chinen H, Hisamatsu T, Hibi T. Tetomilast suppressed production of proinflammatory cytokines from human monocytes and ameliorated chronic colitis in IL-10-deficient mice. Inflamm Bowel Dis. 2008 Nov;14(11):1483-90. doi: 10.1002/ibd.20524. PubMed PMID: 18618633.9: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Sep;29(7):467-509. PubMed PMID: 17982511.10: Keshavarzian A, Mutlu E, Guzman JP, Forsyth C, Banan A. Phosphodiesterase 4 inhibitors and inflammatory bowel disease: emerging therapies in inflammatory bowel disease. Expert Opin Investig Drugs. 2007 Sep;16(9):1489-506. Review. PubMed PMID: 17714033.1
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