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U 46619 (Synonyms: 9,11-dideoxy-9α,11α-methanoepoxy PGF2α, 9,11-dideoxy-9α,11α-methanoepoxy Prostaglandin F2α)

Katalog-Nr.GC13205

Selektiver Agonist des PGH2/TxA2 (TP) Rezeptors

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U 46619 Chemische Struktur

Cas No.: 56985-40-1

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

Protocol

Cell experiment [1]:

Cell lines

Human platelet

Preparation method

Soluble in methyl acetate (supplied pre-dissolved -10 mg/ml). General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

24 h

Applications

In human platelet, U 46619 induced serotonin release, platelet aggregation, and fibrinogen receptor with the EC50 values of 0.54 ± 0.13, 1.31 ± 0.34 and 0.53 ± 0.21 μM, respectively.

Animal experiment [2]:

Animal models

Conscious spontaneously hypertensive rats (SHR)

Dosage form

Intracerebroventricular (ICV) administration, 1–100 nmol/kg

Application

In conscious spontaneously hypertensive rats (SHR), U-46619 (1–100 nmol/kg i.c.v.) induced a strong dose-related increase in blood pressure but had no significant effect on heart rate. In conscious noruotensive rats (NR) neither blood pressure nor heart rate was significantly affected. Furthermore, U-46619 (0.1–100 nmol/kg, i.c.v.) had no significant effect on blood pressure, heart rate or ventilation in urethane-anaesthetised NR .

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

Background

EC50: 0,035 μM für Formveränderung, 0,057 μM für MLCP, 0,536 μM für Serotonin-Freisetzung, 1,31 μM für Aggregation und 0.53 μM für Fibrinogen-Rezeptorbindung [3].

Das Prostaglandin-Endoperoxid-Analogon U46619 (11,9-Epoxymethano-Prostaglandin H2) ist ein selektiver Agonist des Prostaglandin-H2 (PGH2)/Thromboxan-A2 (TxA2) (TP)-Rezeptors. Sowohl PGH2 als auch TxA2-Rezeptoren sind G-Protein gekoppelte Rezeptoren.

In vitro: U46619 zeigte eine biphasische Wirkung auf menschliche Blutplättchen. Formveränderungen und MLCP traten bei niedrigen Konzentrationen dieses Stoffes auf (EC50 = 0,035 uM und 0,057 uM), während Serotoninfreisetzung und Plättchen bei höheren Konzentrationen auftraten (EC50 = 0,536 uM und 1,31 uM). Die Wirkung auf die Formveränderung der Blutplättchen und MLCP ist rezeptorvermittelt [3].

In vivo: U46619 bewirkt durch Aktivierung der ETA- und ETB-Rezeptoren eine Vasokonstriktion in der kortikalen Niere und eine Vasodilatation im Mark bei Ratten [2]. Bei bewussten spontan hypertensiven Ratten (SHR) führte die Verabreichung von 1-100 nmol/kg U-46619 (i.c.v.) zu einer dosisabhängigen Erhöhung des Blutdrucks, hatte jedoch keine signifikante Auswirkung auf die Herzfrequenz [1].

Klinische Studie: Bisher wurde noch keine klinische Studie durchgeführt.

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.

Chemical Properties

Cas No. 56985-40-1 SDF
Überlieferungen 9,11-dideoxy-9α,11α-methanoepoxy PGF2α, 9,11-dideoxy-9α,11α-methanoepoxy Prostaglandin F2α
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
Canonical SMILES O[C@@H](CCCCC)/C=C\[C@@H]1[C@@H](C/C=C/CCCC(O)=O)[C@H]2C[C@H]1OC2
Formula C21H34O4 M.Wt 350.5
Löslichkeit 100 mg/ml in ethanol, DMSO, DMF Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.
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Related Video

    U 46619-GlpBio

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