>>Signaling Pathways>> GPCR/G protein>> Prostaglandin Receptor>>U 46619

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

Catalog No.GC13205

PGH2/TxA2 (TP) 수용체의 선택적 작용제

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U 46619 Chemical Structure

Cas No.: 56985-40-1

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10mg
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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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: 형태 변화에 대해 0.035 μM, MLCP에 대해 0.057 μM, 세로토닌 방출에 대해 0.536 μM, 응집에 대해 1.31 μM 및 피브리노겐 수용체 결합에 대해 0.53 μM [3].

프로스타글란딘 엔도페룩사이드 아날로그 U46619 (11,9 에폭시메탄-프로스타글란딘 H2)은 프로스타글란딘 H2 (PGH2)/트롬보전 A2 (TxA2) (TP) 수용체의 선택적 작용제입니다. PGH2와 TxA2 수용체 모두 G 단백질 결합 수용체입니다.

체외에서: U46619는 인간 혈소판에 양상 변화와 MLCP(biphasic effect)를 보였습니다. 이 화합물의 저 농도(EC50 = 0.035 uM 및 0.057 uM)에서 일어납니다. 반면, 고농도(EC50 = 0.536 uM 및 1.31 uM)에서 혈소판의 세로토닌 방출과 혈소판 효과가 나타납니다. 혈소판 양상 변화와 MLCP에 대한 영향은 수용체 매개입니다 [3].

In vivo: U46619은 ETA 및 ETB 수용체의 활성화를 통해 쥐에서 신장 피질 협착과 골수형 혈관확장을 유도합니다. 의식 중인 SHR(자발적 고혈압쥐)에서 1-100 nmol/kg U-46619 (i.c.v.)는 용량 관련된 혈압 상승을 유도하지만 심박수에는 유의미한 영향이 없습니다.

임상 시험: 지금까지 어떤 임상 연구도 진행되지 않았습니다.

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
Synonyms 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.
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. )

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Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Related Video

    U 46619-GlpBio

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