別品名 |
3-[4-(1H-imidazol-1-ylmethyl)phenyl]-2E-propenoic acid, OKY-046
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別包装 |
あり
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純度 |
>=98%
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分子量 |
264.71
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CAS RN® |
82571-53-7
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化合物の概要 |
TxA2 synthase inhibitor.
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構造 |
C13H12N2O2 HCl
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使用目的 |
Ozagrel is an inhibitor of thromboxane A2 (TxA2) synthase that displays antithrombotic, anti-asthma, and anti-allergic activities. In vivo, ozagrel decreases airway responses to inhalation of leukotriene C4 (LTC4) and TxA2 analog STA2, inhibiting secondary release of TxA2. In other animal models of bronchoconstriction, ozagrel increases levels of prostaglandin I2 (PGI2), inhibiting histamine release. In clinical settings, ozagrel decreases airway contraction in subjects with exercise-induced asthma. In diabetic mice, this compound inhibits retinal arteriolar constriction, preventing decreases in retinal blood flow associated with diabetes-induced retinopathy. Additionally, ozagrel displays cardioprotective activity, decreasing infarct size and thrombus formation in animal models of ischemia-induced myocardial injury. Ozagrel is also hepatoprotective, inhibiting expression of Jun, Fos, and C/EBP homologous protein (CHOP), preventing acetaminophen-induced liver injury.
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参考文献 |
Sathler PC, Santana M, Lourenco AL, et al. Human thromboxane synthase: comparative modeling and docking evaluation with the competitive inhibitors Dazoxiben and Ozagrel. J Enzyme Inhib Med Chem. 2013 Aug 5. Epub ahead of print. PMID: 23914925.Tomishima Y, Ishitsuka Y, Matsunaga N, et al. Ozagrel hydrochloride, a selective thromboxane A2 synthase inhibitor, alleviates liver injury induced by acetaminophen overdose in mice. BMC Gastroenterol. 2013 Jan 30;13:21. PMID: 23363429.Lee S, Morgan GA, Harris NR. Ozagrel reverses streptozotocin-induced constriction of arterioles in rat retina. Microvasc Res. 2008 Nov;76(3):217-23. PMID: 18718478.Fujimura M, Ogawa H, Saito M, et al. Inhibitory effect of inhalation of a thromboxane synthetase inhibitor on bronchoconstriction induced by aerosolized leukotriene C4 and thromboxane A2 analogue in anesthetized guinea pigs. Allergy. 1991 Oct;46(7):534-9. PMID: 1796779.Hoshino M, Fukushima Y. Effect of OKY-046 (thromboxane A2 synthetase inhibitor) on exercise-induced asthma. J Asthma. 1991;28(1):19-29. PMID: 1849133.Nambu F, Murakata S, Shiraji T, et al. OKY-046 inhibits anaphylactic bronchoconstriction and reduces histamine level in bronchoalveolar lavage fluid in sensitized guinea pigs. Prostaglandins. 1990 Jun;39(6):623-37. PMID: 1695383.Tomoda H. Development of an experimental model of acute myocardial infarction and the effects of a thromboxane synthetase inhibitor (OKY-046). Am Heart J. 1986 Oct;112(4):696-704. PMID: 3532743.
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メーカー |
品番 |
包装 |
LKT
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O9702
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10 MG
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※表示価格について
当社在庫 |
なし
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納期目安 |
1週間程度
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保存温度 |
常温
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