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Prostaglandin E2 (PGE2) Prostaglandin Receptor agonist

Cat.nr.: S3003

Prostaglandin E2 (PGE2, Dinoprostone) speelt een belangrijke rol bij de bevalling (verzacht de baarmoederhals en veroorzaakt baarmoedercontracties) en stimuleert ook osteoblasten om factoren vrij te geven die botresorptie door osteoclasten stimuleren. Het is gemakkelijk te verkleuren wanneer het lange tijd in een vloeibare omgeving wordt bewaard. Het wordt aanbevolen om het in poedervorm te bewaren en zo snel mogelijk te gebruiken!
Prostaglandin E2 (PGE2) PGES Chemisch Chemical Structure

Chemische structuur

Molecuulgewicht: 352.47

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: >97.00%
97.00

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving PMID
HeLa Function assay TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, Km = 0.094 μM. 7754369
HeLa Function assay TP_TRANSPORTER: uptake in PGT-expressing HeLa cells, K1/2 = 0.1 μM. 8787677
S2 Function assay TP_TRANSPORTER: uptake in OCT2-expressing S2 cells, Km = 0.0289 μM. 11907186
S2 Function assay TP_TRANSPORTER: uptake in OAT4-expressing S2 cells, Km = 0.154 μM. 11907186
S2 Function assay TP_TRANSPORTER: uptake in OAT3-expressing S2 cells, Km = 0.345 μM. 11907186
S2 Function assay TP_TRANSPORTER: uptake in OCT1-expressing S2 cells, Km = 0.657 μM. 11907186
S2 Function assay TP_TRANSPORTER: uptake in OAT2-expressing S2 cells, Km = 0.713 μM. 11907186
S2 Function assay TP_TRANSPORTER: uptake in OAT1-expressing S2 cells, Km = 0.97 μM. 11907186
HEK293 Function assay Inhibitory activity against human EP4 receptor expressed in HEK293 ebna cells, IC50 = 0.0007 μM. 12643927
HEK293 Function assay EP4 agonist potency utilizing a stable clone of pSV40-EP4 transfected into HEK293 cells expressing EP4 receptor, EC50 = 0.003 μM. 12643927
Sf9 Function assay TP_TRANSPORTER: uptake (vesicle) in membrane vesicles from MRP4-expressing Sf9 cells, Km = 3.4 μM. 12835412
HEK293 Function assay Displacement of [3H]PGE2 from human EP3 receptor expressed in HEK293 cells, Ki = 0.00033 μM. 17531488
HEK293 Function assay Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells, Ki = 0.00079 μM. 17531488
HEK293 Function assay Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells, Ki = 0.0049 μM. 17531488
HEK293 Function assay Displacement of [3H]PGE2 from human EP1 receptor expressed in HEK293 cells, Ki = 0.0091 μM. 17531488
HEK293 Function assay Agonist activity against rat EP2 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0002 μM. 19250823
HEK293 Function assay Agonist activity against rat EP4 receptor expressed in HEK293 cells assessed as stimulation of cAMP release, EC50 = 0.0007 μM. 19250823
HEK293 Function assay Inhibition of rat EP4 receptor expressed in HEK293 cells, IC50 = 0.0021 μM. 19250823
HEK293 Function assay Inhibition of rat EP2 receptor expressed in HEK293 cells, IC50 = 0.0052 μM. 19250823
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.0031 μM. 22119471
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.005 μM. 22119471
CHO Function assay 20 mins Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 20 mins by liquid scintillation counting, Ki = 0.006 μM. 22119471
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting, Ki = 0.022 μM. 22119471
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.0031 μM. 22386979
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP3 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.005 μM. 22386979
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP1 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.006 μM. 22386979
CHO Function assay 60 mins Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by scintillation counting, Ki = 0.022 μM. 22386979
CHEM1 Function assay 2 hrs Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, Ki = 0.00045 μM. 23403082
CHEM1 Function assay 2 hrs Displacement of [3H]PGE2 from human recombinant prostanoid EP4 receptor in CHEM1 cells after 2 hrs, IC50 = 0.0011 μM. 23403082
CHO Function assay 100 nM Activity at recombinant EP1 receptor (unknown origin) expressed in CHO cells co-expressing Gq protein at 100 nM by electrical cell substrate impedance sensing system 25701254
CHO Function assay 100 nM Activity at recombinant EP4 receptor (unknown origin) expressed in CHO cells co-expressing Gs protein at 100 nM by electrical cell substrate impedance sensing system 25701254
CHO Function assay 100 nM Activity at recombinant EP3 receptor (unknown origin) expressed in CHO cells co-expressing Gi protein at 100 nM by electrical cell substrate impedance sensing system 25701254
CHO Function assay 30 mins Agonist activity at human EP2 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0019 μM. 26985320
CHO Function assay Agonist activity at human EP3 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0025 μM. 26985320
CHO Function assay Agonist activity at human EP1 receptor expressed in CHO cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.0037 μM. 26985320
CHO Function assay 30 mins Agonist activity at human EP4 receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.0075 μM. 26985320
Chem1 Function assay Agonist activity at human FP receptor expressed in human Chem1 cells assessed as increase in intracellular calcium level by fluorescence based analysis, EC50 = 0.25 μM. 26985320
HEK293 Function assay 90 mins Agonist activity at PK2-tagged human EP2 receptor expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin recruitment incubated for 90 mins by beta-galactosidase reporter gene assay, EC50 = 0.346 μM. 26985320
CHO Function assay 30 mins Agonist activity at human IP receptor expressed in CHO cells assessed as increase in intracellular cAMP level after 30 mins by HTRF method, EC50 = 0.347 μM. 26985320
HEK293 Function assay Displacement of [3H]PGE2 from human recombinant prostanoid EP2 receptor expressed in HEK293 cells, IC50 = 0.0026 μM. 26988801
HEK293 Function assay 120 mins Displacement of [3H]PGE2 from human recombinant EP4 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.00055 μM. 27876250
HEK293 Function assay 120 mins Displacement of [3H]PGE2 from human recombinant EP2 receptor expressed in HEK293 cells measured after 120 mins by scintillation counting method, IC50 = 0.0026 μM. 27876250
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 352.47 Formule

C20H32O5

Opslag (vanaf de datum van ontvangst)
CAS-nr. 363-24-6 SDF downloaden Opslag van stamoplossingen Oplossingen zijn instabiel. Bereid ze vers of koop kleine, voorverpakte formaten. Herverpakken na ontvangst.
Synoniemen Dinoprostone Smiles CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 70 mg/mL (198.59 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 70 mg/mL

Water : 2.5 mg/mL

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

In vitro

PGE2 acts via EP4 receptors on osteoclasts during the progression of OA and OA-related pain.

In vivo

PGE2 (0.3 μg/k, i.p.) significantly reduces the number of peritoneab macrophages undergoing phagocytosis of the methacrybate microbeads in rats.

Referenties

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer Werving Aandoeningen Sponsor/medewerkers Startdatum Fasen
NCT06129604 Recruiting
Colorectal Carcinoma (CRC)|Endometrial Carcinoma (EC)
University of Oklahoma
April 3 2024 Phase 2
NCT06307678 Completed
Periapical; Infection
Ataturk University
July 7 2023 Not Applicable
NCT06190132 Completed
Uremic Pruritus in Hemodialysis Patients
Ain Shams University
April 1 2023 Not Applicable