切换导航

U 46619

现货
Catalog No.
B6890
前列腺素H2(PGH2)/血栓素A2(TxA2)(TP)受体激动剂
组合的产品项目
规格价格库存 数量
1mg
¥ 700.00
Please inquiry
5mg
¥ 3,150.00
Please inquiry
10mg
¥ 5,600.00
Please inquiry

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

EC50: 0.035 μM for shape change, 0.057 μM for MLCP, 0.536 μM for serotonin release, 1.31 μM for aggregation and 0.53 μM for fibrinogen receptor binding [3].

Prostaglandin endoperoxide analogue U46619 (11,9 epoxymethano-prostaglandin H2) is a selective agonist of prostaglandin H2 (PGH2)/thromboxane A2 (TxA2) (TP) receptor. Both PGH2 and TxA2 receptors are G-protein coupled receptors.

In vitro: U46619 showed a biphasic effect on human platelets. Shape change and MLCP occurred at low concentrations of this compound (EC50 = 0.035 uM and 0.057 uM), whereas serotonin release, platelet at higher concentrations (EC50 = 0.536 uM and 1.31 uM). The effect on platelet shape change and MLCP is receptor mediated [3].

In vivo:. U46619, through activation of ETA and ETB receptors, elicits renal cortical vasoconstriction and medullary vasodilation in the rat [2]. In conscious SHR (spontaneously hypertensive rats), 1-100 nmol/kg U-46619 (i.c.v.) induced a dose-related increase in blood pressure but had no significant effect on heart rate [1].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Sirén AL, Svartstrm-Fraser M, Paakkari I.  Central cardiovascular effects of the endoperoxide analogue U-46619 in rats. Prostaglandins Leukot Med. 1985 Mar;17(3):381-6.
[2] Hantz H, Adesuyi A, Adebayo O.  Differential effects of U46619 on renal regional hemodynamics in the rat: involvement of endothelin. J Pharmacol Exp Ther. 2001 Oct;299(1):372-6.
[3] Morinelli TA1, Niewiarowski S, Daniel JL, Smith JB.  Receptor-mediated effects of a PGH2 analogue (U 46619) on human platelets. Am J Physiol. 1987 Nov;253(5 Pt 2):H1035-43.

文献引用

1. Yan YY, Ao LY, et al. "Therapeutic effects of JLX001 on cerebral ischemia through inhibiting platelet activation and thrombus formation in rats." Biomed Pharmacother. 2018 Jul 7;106:805-812. PMID:29990874
2. Zhang Q, Tan CN, et al. "Adsorbed hollow fiber-based biological fingerprinting for the discovery of platelet aggregation inhibitors from Danshen-Honghua decoction." J Sep Sci. 2018 Mar 23. PMID:29573136
3. Zhang Q, Tan C, et al. "Characterization of active antiplatelet chemical compositions of edible Citrus limon through ultra-performance liquid chromatography single quadrupole mass spectrometry-based chemometrics." Food Funct. 2018 Apr 24. PMID:29687827

Chemical Properties

Physical AppearanceA solution in methyl acetate
StorageStore at -20°C
M.Wt350.5
Cas No.56985-40-1
FormulaC21H34O4
SolubilitySoluble in methyl acetate
Chemical Name(E)-7-((1R,4R,5S,6R)-6-((S,Z)-3-hydroxyoct-1-en-1-yl)-2-oxabicyclo[2.2.1]heptan-5-yl)hept-5-enoic acid
SDFDownload SDF
Canonical SMILESO[C@@H](CCCCC)/C=C\[C@@H]1[C@@H](C/C=C/CCCC(O)=O)[C@H]2C[C@H]1OC2
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
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。

试验操作

细胞实验 [1]:

细胞系

人血小板

溶解方法

溶于乙酸甲酯,预先溶解为10 mg/ml。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

24 h

应用

在人血小板中,U46619诱导血清素释放、血小板聚集和纤维蛋白原受体,EC50值分别为0.54 ± 0.13、1.31 ± 0.34和0.53 ± 0.21 μM。

动物实验 [2]:

动物模型

自发性高血压大鼠(SHR)

给药剂量

脑室内(ICV)给药,1–100 nmol/kg

应用

在有意识的自发性高血压大鼠(SHR)中,U-46619(1–100 nmol/kg i.c.v.)引起强烈剂量相关的血压升高,但对心率无明显影响。在有意识的雄性大鼠(NR)中,血压和心率都没有显著受影响。此外,U-46619(0.1–100 nmol/kg i.c.v.)对氨基甲酸酯麻醉NR的血压、心率或通气率无明显影响。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Morinelli T A, Niewiarowski S, Daniel J L, et al. Receptor-mediated effects of a PGH2 analogue (U 46619) on human platelets[J]. American Journal of Physiology-Heart and Circulatory Physiology, 1987, 253(5): H1035-H1043.

[2]. Siren A L, Svartstrm-Fraser M, Paakkari I. Central cardiovascular effects of the endoperoxide analogue U-46619 in rats[J]. Prostaglandins, Leukotrienes and Medicine, 1985, 17(3): 381-386.

质量控制

质量控制和MSDS

批次:

化学结构

U 46619

相关生物数据

U 46619

相关生物数据

U 46619

相关生物数据

U 46619