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Ramatroban

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Chemical Structure| 116649-85-5 同义名 : BAY u3405;​Bay u3405;EN 137774.;Bay u 3406
CAS号 : 116649-85-5
货号 : A436709
分子式 : C21H21FN2O4S
纯度 : 98%
分子量 : 416.466
MDL号 : MFCD00887606
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(288.14 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 Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding. Ramatroban also inhibits human CYP isoform CYP2C9 with an IC50 of 15 μM[3]. Ramatroban, a small-molecule antagonist of DP2 and TP receptors, reverses viremia-associated proinflammatory, immunosuppressive5 and prothrombotic processes which are similar to those induced by SARS-Cov-2[4]. Ramatroban, a dual CRTH2/thromboxane-like prostanoid receptor antagonist, markedly inhibited Th2 cytokine production induced by PGD2, while the selective thromboxane-like prostanoid receptor antagonist SQ29548 was without effect[5]. Ramatroban significantly alleviated silica-induced pulmonary inflammation, fibrosis, and cardiopulmonary dysfunction compared with the control group[6]. Ramatroban similarly inhibited asthma pathology in vivo by reducing peribronchial eosinophilia and mucus cell hyperplasia[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.40mL

0.48mL

0.24mL

12.01mL

2.40mL

1.20mL

24.01mL

4.80mL

2.40mL
参考文献

[1]Ishizuka T, Matsui T, et al. Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. Cardiovasc Drug Rev. 2004 Summer;22(2):71-90.

[2]Sundstrom E, Låstbom L, et al. Interactions among three classes of mediators explain antigen-induced bronchoconstriction in the isolated perfused and ventilated guinea pig lung. J Pharmacol Exp Ther. 2003 Oct;307(1):408-18.

[3]Sugimoto H, Shichijo M, Iino T, Manabe Y, Watanabe A, Shimazaki M, Gantner F, Bacon KB. An orally bioavailable small molecule antagonist of CRTH2, ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther. 2003 Apr;305(1):347-52

[4]Gupta A, Kalantar-Zadeh K, Reddy ST. Ramatroban as a Novel Immunotherapy for COVID-19. J Mol Genet Med. 2020;14(3):10.37421

[5]Xue L, Gyles SL, Wettey FR, Gazi L, Townsend E, Hunter MG, Pettipher R. Prostaglandin D2 causes preferential induction of proinflammatory Th2 cytokine production through an action on chemoattractant receptor-like molecule expressed on Th2 cells. J Immunol. 2005 Nov 15;175(10):6531-6

[6]Pang J, Qi X, Luo Y, Li X, Shu T, Li B, Song M, Liu Y, Wei D, Chen J, Wang J, Wang C. Multi-omics study of silicosis reveals the potential therapeutic targets PGD2 and TXA2. Theranostics. 2021 Jan 1;11(5):2381-2394

[7]Uller L, Mathiesen JM, Alenmyr L, Korsgren M, Ulven T, Högberg T, Andersson G, Persson CG, Kostenis E. Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation. Respir Res. 2007 Feb 28;8(1):16