| U 46619 目录号 GC13205 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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Purity: >98.00%
- COA (Certificate Of Analysis)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Human platelet |
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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. |
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Reacting condition |
24 h |
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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]: | |
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Animal models |
Conscious spontaneously hypertensive rats (SHR) |
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Dosage form |
Intracerebroventricular (ICV) administration, 1–100 nmol/kg |
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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 . |
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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. |
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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. |
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| Cas No. | 56985-40-1 | SDF | |
| 别名 | N/A | ||
| 化学名 | (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 | ||
| 分子式 | C21H34O4 | 分子量 | 350.5 |
| 溶解度 | 100 mg/ml in ethanol, DMSO, DMF | 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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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.