| BAY u3405DP2 receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
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 Three subjects were withdrawn from the evaluation.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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Musmusculus2dayspregnantadultfemaleovaryCDNA,RIKENfull-lengthenrichedlibrary,clone:E330021J16product:inferred:SRY-boxcontaininggene4/sox-4,fullinsertsequence。
product:inferred:SRY-boxcontaininggene4/sox-4,fullinsertsequence是什么意思，这个基因推测产物是sox-4？fullinsertsequence是什么意思？
以前听说过设计引物，以引物互为模板进行PCR获得的引物二聚体就是目的片段
有没有人具体操作过呢？应该注意什么问题呢？比如引物设计，体系，PCR程序
甲苯二异氰酸酯(TDI)有两种异构体:2，4-甲苯二异氰酸酯和2，6-甲苯二异氰酸酯。甲苯二异氰酸酯是水白色或淡黄色液体，具有强烈的刺激性气味，在人体中具有积聚性和潜伏性，对皮肤、眼睛和呼吸道有强烈刺激作用，吸入高浓度的甲苯二异氰酸酯蒸气会引起支气管炎、支气管肺炎和肺水肿;液体与皮肤接触可引起皮炎。液体与眼睛接触可引起严重刺激作用，如果不加以治疗，可能导致永久性损伤。长期接触甲苯二异氰酸酯可引起慢性支气管炎。对甲苯二异氰酸酯过敏者，可能引起气喘、伴气喘、呼吸困难和咳嗽。
与乙醚、二甘醇、丙酮、四氯化碳、苯、氯苯、煤油、橄榄油混溶。能与含羟基的化合物、水、胺和具有活泼氢原子的化合物反应生成氨基甲酸酯、脲、氨基脲等。甲苯用混酸硝化得到2,4-和2,6-二硝基甲苯，然后在镍催化剂存在下加氢还原得到2,4-和2,6-二氨基甲苯，再在氯苯溶液中与光气反应制得。主要作为聚氨酯树脂的生产原料，用于生产聚氯酯泡抹塑料、涂料、橡胶、粘合剂、密封剂等。也可用作橡胶硫化剂、蛋白质交联剂等。包括泡沫塑料;聚氨酯涂料;聚氨酯橡胶;聚酰亚胺纤维和胶粘剂等也有一些应用。有2，4-甲苯二异氰酸酯和2，6-甲苯二异氰酸酯(TDI)两种异构体。按两种异构体含量的不同，工业上有三种规格的产品:(1)TDI-65含2,4-TDI65%，2,6-TDI35%;(2)TDI-80含2,4-TDI80%，2,6-TDI20%，最为常见;(3)TDI-100含2,4-TDI100%。与水作用产生二氧化碳。易与含有活性氢原子的化合物作用。与二元醇作用而成线型聚氨基甲酸酯或聚氨酯树脂。
橡胶的硫化、不饱和树脂的交联、环氧树脂的熟化等都是化学交联的例子。
通过化学交联可改善聚合物的性能。如聚乙烯的化学交联可提高其强度和耐热性，又如皮革的鞣制过程是利用其蛋白质分子与甲醛作用，生成交联桥，以至失去溶解性。
