U 46619 (Synonyms: 9,11-dideoxy-9α,11α-methanoepoxy PGF2α, 9,11-dideoxy-9α,11α-methanoepoxy Prostaglandin F2α) |
Catalog No.GC13205 |
Sélectif agoniste du récepteur PGH2/TxA2 (TP)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 56985-40-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
EC50 : 0,035 μM pour le changement de forme, 0,057 μM pour MLCP, 0,536 μM pour la libération de sérotonine, 1,31 μM pour l'agrégation et 0.53 μM pour la liaison au récepteur du fibrinogène [3].
L'analogie de l'endoperoxyde de prostaglandine U46619 (11,9 époxy-méthano-prostaglandine H2) est un agoniste sélectif du récepteur d'H2 de la prostaglandine (PGH2)/thromboxane A2 (TxA2) (TP). Les deux récepteurs PGH2 et TxA2 sont des récepteurs couplés à une protéine G.
In vitro : U46619 a montré un effet biphasique sur les plaquettes humaines. Le changement de forme et la MLCP se sont produits à faibles concentrations de ce composé (EC50 = 0,035 uM et 0,057 uM), tandis que la libération de sérotonine et l'agrégation des plaquettes ont eu lieu à des concentrations plus élevées (EC50 = 0,536 uM et 1,31 uM). L'effet sur le changement de forme des plaquettes et la MLCP est médié par les récepteurs [3].
In vivo: U46619, par l'activation des récepteurs ETA et ETB, provoque une vasoconstriction corticale rénale et une vasodilatation médullaire chez le rat [2]. Chez les rats spontanément hypertendus conscients (SHR), 1-100 nmol/kg de U-46619 (i.c.v.) a induit une augmentation dose-dépendante de la pression artérielle mais n'a eu aucun effet significatif sur la fréquence cardiaque [1].
Essai clinique : Jusqu'à présent, aucune étude clinique n'a été menée.
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.
Cas No. | 56985-40-1 | SDF | |
Synonymes | 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. |
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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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
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