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Seratrodast

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Chemical Structure| 112665-43-7 同义名 : AA 2414;A-73001;CCRIS 8939.;Abbott 73001;ABT-001
CAS号 : 112665-43-7
货号 : A246719
分子式 : C22H26O4
纯度 : 98%
分子量 : 354.44
MDL号 : MFCD00875701
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(296.24 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Thromboxane synthase (TXAS) is a P450 epoxygenase that synthesizes thromboxane A2 (TXA2), a potent mediator of platelet aggregation, vasoconstriction and bronchoconstriction[3]. Seratrodast (AA 2414) is an anti-asthmatic agent and a potent and selective thromboxane A2 receptor (TP) antagonist[4]. Seratrodast inhibited peroxide-induced vasoconstriction in the human placenta, as well as peroxide- induced increases in the placental secretion rates of lipid peroxides and thromboxane, but only partially inhibited peroxide-induced increases in the placental secretion rate of prostacyclin[5]. Seratrodast reduced the overproduction of TxB2 in both bronchoalveolar lavage fluid and lung tissues. Cigarette smoke exposure markedly increased AB/PAS-stained goblet cells and rat Muc5ac expression in the airway, which was significantly attenuated by seratrodast administration. The induced phosphorylation of ERK and p38 was also attenuated by seratrodast[6]. The anti-asthmatic activity of AA-2414 has been studied in vivo and in vitro. Experimental allergic asthma was inhibited by orally administered AA-2414 in a dose-dependent manner. AA-2414, 0.08-1.25 mg/kg (p.o.), inhibited the bronchconstriction in guinea pigs induced by a prostaglandin endoperoxide analogue (U-46619), leukotriene D4 (LTD4), and platelet activating factor (PAF) with a long duration of action. The compound did not inhibit histamine-induced bronchoconstriction. AA-2414 reduced the induction of pulmonary inflation caused by LTD4 aerosol inhalation. AA-2414 competitively inhibited the contractile response to U-46619 in guinea pig tracheal and parenchymal strips and dog saphenous vein strips with pA2 values of 7.69, 8.29 and 6.79, respectively[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02716246 Mucopolysaccharidosis Type 3 A... 展开 >> Sanfilippo Syndrome 收起 << Phase 1 Phase 2 Recruiting December 2020 United States, Ohio ... 展开 >> Nationwide Children's Hospital Recruiting Columbus, Ohio, United States, 43205 Contact: Krista Kunkler    614-722-2238    krista.kunkler@nationwidechildrens.org    Australia, South Australia Women's and Children's Hospital Recruiting North Adelaide, South Australia, Australia, 5006 Contact: Louise Jaensch    08 8161 7295    louise.jaensch@sa.gov.au    Principal Investigator: Nicholas Smith, MD          Spain Hospital Clínico Universitario de Santiago Recruiting Santiago De Compostela, Spain, 15706 Contact: Maria Luz Couce, MD    +34 981 950 151    maria.luz.couce.pico@sergas.es    Contact: Maria Jose de Castro, MD    +34 981 955 627    maria.jose.de.castro.lopez@sergas.es 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.82mL

0.56mL

0.28mL

14.11mL

2.82mL

1.41mL

28.21mL

5.64mL

2.82mL
参考文献

[1]Kurokawa T, Matsumoto T, et al. Antagonism of the human thromboxane A2 receptor by an anti-asthmatic agent AA-2414. Biol Pharm Bull. 1994 Mar;17(3):383-5.

[2]Ashida Y, Matsumoto T, et al. A novel anti-asthmatic quinone derivative, AA-2414 with a potent antagonistic activity against a variety of spasmogenic prostanoids. Prostaglandins. 1989 Jul;38(1):91-112.

[3]Plínio Cunha Sathler,et al. Human thromboxane synthase: comparative modeling and docking evaluation with the competitive inhibitors Dazoxiben and Ozagrel. J Enzyme Inhib Med Chem. 2014 Aug;29(4):527-31.

[4]Ashida, Y., et al., A novel anti-asthmatic quinone derivative, AA-2414 with a potent antagonistic activity against a variety of spasmogenic prostanoids. Prostaglandins, 1989. 38(1): p. 91-112.

[5]S W Walsh,et al. AA-2414, an antioxidant and thromboxane receptor blocker, completely inhibits peroxide-induced vasoconstriction in the human placenta. J Pharmacol Exp Ther. 1999 Jul;290(1):220-6.

[6]Jing An,et al. Blocking of thromboxane A₂ receptor attenuates airway mucus hyperproduction induced by cigarette smoke. Eur J Pharmacol. 2013 Mar 5;703(1-3):11-7.

[7]Y Ashida,et al. A novel anti-asthmatic quinone derivative, AA-2414 with a potent antagonistic activity against a variety of spasmogenic prostanoids. Prostaglandins.1989 Jul;38(1):91-112.