U 46619
(Synonyms: 9,11-二脱氧基-9Α,11Α-亚甲基环氧前列腺素F2Α溶液,9,11-Methanoepoxy PGH2) 目录号 : GC13205A TP receptor agonist
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]: | |
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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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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.
| Cas No. | 56985-40-1 | SDF | |
| 别名 | 9,11-二脱氧基-9Α,11Α-亚甲基环氧前列腺素F2Α溶液,9,11-Methanoepoxy PGH2 | ||
| 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 | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8531 mL | 14.2653 mL | 28.5307 mL |
| 5 mM | 0.5706 mL | 2.8531 mL | 5.7061 mL |
| 10 mM | 0.2853 mL | 1.4265 mL | 2.8531 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。