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BAY u3405
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BAY u3405图片
CAS NO:116649-85-5
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt416.5
Cas No.116649-85-5
FormulaC21H21FN2O4S
SynonymsRamatroban
Solubility≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical Name3R-[[(4-fluorophenyl)sulfonyl]amino]-1,2,3,4-tetrahydro-9H-carbazole-9-propanoic acid
Canonical SMILESO=S(N[C@H](CC1)CC2=C1N(CCC(O)=O)C3=CC=CC=C23)(C4=CC=C(F)C=C4)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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 Three subjects were withdrawn from the evaluation.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.