| BAY u3405DP2 receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 116649-85-5 | SDF | Download SDF |
| Synonyms | Ramatroban | ||
| Chemical Name | 3R-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid | ||
| Canonical SMILES | O=S(N[C@H](CC1)CC2=C1N(CCC(O)=O)C3=CC=CC=C23)(C4=CC=C(F)C=C4)=O | ||
| Formula | C21H21FN2O4S | M.Wt | 416.5 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 100-170 nM
BAY u3405 is a DP2 receptor antagonist.
The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and DP2/CRTH2.
In vitro: BAY u3405 showed significant inhibitory effects on the binding of 3H-labeled PGD2 to CRTH2, albeit with much lower potency. BAY u3405 and indomethacin also inhibited PGD2-induced Ca2+ mobilization in CRTH2 transfectants to almost the same extent. However, indomethacin but not BAY u3405 was confirmed as an agonist of Ca2+ mobilization at concentrations greater than 10 nM [1].
In vivo: For rat with splanchnic artery occlusion shock, administration of BAY u3405 at 30 mg/kg i.v. could significantly increase the survival time and survival rate, improve mean arterial blood pressure, reduce the plasma levels of myocardial depressant factor, partially restore macrophage phagocytosis and lower MPO activity in both the ileum and the lung [2].
Clinical trial: Twelve adult asthmatics were studied in a randomized, double-blind, placebo-controlled study. Three subjects were withdrawn from the evaluation. The Dmin value of 0.533 U after the BAY u3405 treatment was significantly greater than that of 0.135 U after the placebo treatment. There were no safety concerns in either treatment group [3].
References:[1] Sugimoto, H.,Shichijo, M.,Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. Journal of Pharmacology and Experimental Therapeutics 305, 347-352 (2003).[2] Canale P, Squadrito F, Altavilla D, Ioculano M, Campo GM, Squadrito G, Urna G, Sardella A, Caputi AP. Beneficial effects of BAY u3405, a novel thromboxane A2 receptor antagonist, in splanchnic artery occlusion shock. Pharmacology. 1994 Dec;49(6):376-85.[3] Aizawa H, Shigyo M, Nogami H, Hirose T, Hara N.BAY u3405, a thromboxane A2 antagonist, reduces bronchial hyperresponsiveness in asthmatics. Chest. 1996 Feb;109(2):338-42.
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2017年4月26日|Filedunder:制药工业,制药企业,孤儿药,新药研发,制药常识,文献综合|Postedby:路人丙
【新闻事件】：在日前正在举行的美国神经学年会上MitsubishiTanabe公布了其ALS药物Edaravone的一个三期临床试验结果。在标准疗法基础上加入Edaravone显著改善ALS患者综合功能指标ALSFRS-R（-5.0对-7.5），同时也改善运动、呼吸等局部功能。Edaravone已经在韩国日本批准用于ALS，去年10月申请在美国上市，今年6月之前有望批准。
【药源解析】：ALS全称叫“肌肉萎缩性侧面硬化病”，也称LouGehrig氏病，因为30年代美国纽约洋基棒球队著名选手LouGehrig死于这个病。2014年风行一时的冰桶挑战让更多人知道了ALS，但ALS新药发现依然缓慢。美国目前只有riluzole这一个上市药物，能增加~10%的一年生存机会。
ALS的发病机理未知，动物模型十分不可靠，所以这个病的新药开发很难。过去10年大约只有十几个药物进入临床，基本全军覆没。走的最远的是百建艾迪的dexpramipexole，2013年初在三期临床失败。Edaravone号称是游离基清除剂，但分子机理未知。Edaravone最早作为中风药物开发，后来扩展到ALS。第一个三期临床失败，今天公布的是症状较轻患者。这个临床是日本人群，Edaravone并没有在美国IND和开展临床试验，所以如果批准将是比较特殊的情况（和Marathon的DMD药物Emflaza情况类似）。
Edaravone的另一个特殊性质是其分子结构。这个化合物分子十分简单，分子量只有174，可以算作是超小分子药物。现在有几十个分子量小于200的FDA批准药物，这类药物因为官能团数目有限不大可能与任何靶点有较高结合能，所以通常靶点未知。靶点未知又没有可靠动物模型，这类药物发现就更加困难。当然动物模型预测性差不是超小分子药物才面临的难题，多数神经系统药物、甚至现在最火热的肿瘤免疫疗法也面临同样问题。
这种临床前缺乏可靠评价体系的药物可以算是有D无R，这要求厂家冒更大的临床风险。只有潜在回报较大如没有任何标准疗法的罕见病或真正颠覆性药物如免疫疗法才可以适当采用这个模式。这个模式扩大化对厂家的长期生存是个威胁，因为新药的未知因素已经很多、成功率已经很低。没有临床前适当去风险的机会主义不可持续。
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美中药源原创文章，转载注明出处并添加超链接，商业用途需经书面授权。
★更多深度解析访问《美中药源》~
https://www.yypharm.com/?p=10664
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