| 5-trans U-46619Prostaglandin E synthase inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 330796-58-2 | SDF | Download SDF |
| Synonyms | 5,6-trans U-46619 | ||
| Chemical Name | 9,11-dideoxy-9α,11α-methanoepoxy-prosta-5E,13E-dien-1-oic acid | ||
| Canonical SMILES | CCCCC[C@H](O)/C=C/[C@H]1C2OCC(C2)[C@@H]1C/C=C/CCCC(O)=O | ||
| Formula | C21H34O4 | M.Wt | 350.5 |
| Solubility | ≤100mg/ml in ethanol;100mg/ml in DMSO;100mg/ml in dimethyl formamide;2mg/ml in PBS(pH7.2) | Storage | Store at -20°C |
| Physical Appearance | A solution in methyl acetate | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
5-trans U-46619 is a minor impurity (2-5%) which variably exists in most commercial preparations of U-46619 [1]. U-46619 is a selective thromboxane A2 agonist involved in inducing platelet aggregation and vascular smooth muscle contraction [2].
The biological activity of 5-trans U-46619 has been rarely tested separately from U-46619 itself. In the only case published to date, 5-trans U-46619 was found to be a about half as potent an inhibitor of Prostaglandin E synthase as the 5-cis version of U-46619 [1]. Thromboxane A2 (TxA2) has been involved in the pathogenesis of airway hyperresponsiveness. TXA2 is a type of thromboxane produced by activated platelets and shows prothrombotic properties. Thromboxane A2 has also been known as a vasoconstrictor and is especially important during tissue injury and inflammation [3].
References:[1] Quraishi O, Mancini J A, Riendeau D. Inhibition of inducible prostaglandin E 2 synthase by 15-deoxy-Δ 12, 14-prostaglandin J 2 and polyunsaturated fatty acids[J]. Biochemical pharmacology, 2002, 63(6): 1183-1189.[2] Coleman, R.A.,Humphrey, P.P.A.,Kennedy, I., et al. Comparison of the actions of U-46619, a prostaglandin H2-analogue, with those of prostaglandin H2 and thromboxane A2 on some isolated smooth muscle preparations. British Journal of Pharmacology 73, 773-778 (1981).[3] Svensson J, Strandberg K, Tuvemo T, et al. Thromboxane A2: Effects of airway and vascular smooth muscle[J]. Prostaglandins, 1977, 14(3): 425-436.
