Home Endocrinology & Hormones PGES chemical Prostaglandin E2 (PGE2)

solo per uso di ricerca

Prostaglandin E2 (PGE2) Prostaglandin E Receptor agonist

N. Cat.: S3003

Prostaglandin E2 (PGE2, Dinoprostone) plays important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts. It is easy to discolor when stored in liquid environment for a long time. It is recommended to store it in powder form and try to use it as soon as possible!
Prostaglandin E2 (PGE2) PGES chemical Chemical Structure

Struttura chimica

Peso molecolare: 352.47

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: >97.00%
97.00

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari Tipo di saggio Concentrazione Tempo di incubazione Formulazione Descrizione dell'attività 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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare 352.47 Formula

C20H32O5

 Conservazione (Dalla data di ricezione)
N. CAS 363-24-6 Scarica SDF Conservazione delle soluzioni stock Le soluzioni sono instabili. Preparare al momento o acquistare formati piccoli e preconfezionati. Riconfezionare al ricevimento.
Sinonimi Dinoprostone Smiles CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 70 mg/mL (198.59 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 70 mg/mL

Water : 2.5 mg/mL

Calcolatore di Molarità

Massa Concentrazione Volume Peso molecolare
Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo
Lotto:

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

mg/kg g μL

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH2O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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.
Riferimenti

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT Reclutamento Condizioni Sponsor/Collaboratori Data di inizio Fasi
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