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

カタログ番号GC13205

PGH2/TxA2(TP)受容体の選択的アゴニスト

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U 46619 化学構造

Cas No.: 56985-40-1

サイズ 価格 在庫数 個数
1mg
$135.00
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5mg
$570.00
在庫あり
10mg
$1,004.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

View current batch:

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値:形状変化に対して0.035μM、MLCPに対して0.057μM、セロトニン放出に対して0.536μM、凝集に対して1.31μM、フィブリノーゲン受容体結合に対して0.53μM [3]。

プロスタグランジンエンドペルオキシドアナログU46619(11,9-エポキシメタノ-プロスタグランジンH2)は、プロスタグランジンH2(PGH2)/トロンボキサンA2(TxA2)(TP)受容体の選択的アゴニストです。 PGH2およびTxA2受容体は両方ともGタンパク質共役受容体です。

体外実験:U46619は、人間の血小板に対して二相性の効果を示しました。この化合物の低濃度(EC50 = 0.035 uMおよび0.057 uM)では形状変化とMLCPが起こりますが、高濃度ではセロトニン放出や血小板などが起こります(EC50 = 0.536 uMおよび1.31 uM)。血小板の形状変化とMLCPに対する影響は受容体媒介です[3]。

生体内:U46619は、ETAおよびETB受容体の活性化を介して、ラットにおいて腎皮質血管収縮と髄質血管拡張を引き起こす[2]。自発的高血圧ラット(SHR)では、意識下で1-100 nmol/kgのU-46619(i.c.v.)が投与されると、用量依存的に血圧が上昇するが心拍数に有意な影響はなかった[1]。

臨床試験:現時点では、まだ臨床研究は行われていません。

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
同義語 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
溶解度 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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計算

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Related Video

    U 46619-GlpBio

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