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

Catalog No.GC13205

Agonista selectivo del receptor PGH2/TxA2 (TP).

Products are for research use only. Not for human use. We do not sell to patients.

U 46619 Chemical Structure

Cas No.: 56985-40-1

Tamaño Precio Disponibilidad Cantidad
1mg
135,00 $
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5mg
570,00 $
Disponible
10mg
1.004,00 $
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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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 para cambio de forma, 0.057 μM para MLCP, 0.536 μM para liberación de serotonina, 1.31 μM para agregación y 0.53 μM para unión al receptor de fibrinógeno [3].

El análogo de la endoperóxido prostaglandina U46619 (11,9 epoximetano-prostaglandina H2) es un agonista selectivo del receptor de la prostaglandina H2 (PGH2)/tromboxano A2 (TxA2) (TP). Tanto los receptores PGH2 como TxA2 son receptores acoplados a proteínas G.

En vitro: U46619 mostró un efecto bifásico en las plaquetas humanas. El cambio de forma y la MLCP ocurrieron a bajas concentraciones de este compuesto (EC50 = 0,035 uM y 0,057 uM), mientras que la liberación de serotonina y las plaquetas se produjeron a concentraciones más altas (EC50 = 0,536 uM y 1,31 uM). El efecto sobre el cambio de forma de las plaquetas y la MLCP es mediado por receptores [3].

En vivo: U46619, a través de la activación de los receptores ETA y ETB, provoca vasoconstricción cortical renal y vasodilatación medular en ratas [2]. En SHR conscientes (ratones hipertensos espontáneos), 1-100 nmol/kg U-46619 (i.c.v.) indujo un aumento relacionado con la dosis en la presión arterial pero no tuvo un efecto significativo sobre la frecuencia cardíaca [1].

Ensayo clínico: Hasta ahora, no se ha llevado a cabo ningún estudio clínico.

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
Sinónimos 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
Solubility 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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