réservé à la recherche
N° Cat.S3003
| Cibles apparentées | Adrenergic Receptor Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR |
|---|---|
| Autre PGES Inhibiteurs | Yakuchinone A |
| Lignées cellulaires | Type dessai | Concentration | Temps dincubation | Formulation | Description de lactivité | 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 | ||
| Cliquez pour voir plus de données expérimentales sur les lignées cellulaires | ||||||
| Poids moléculaire | 352.47 | Formule | C20H32O5 |
Stockage (À partir de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 363-24-6 | Télécharger le SDF | Stockage des solutions mères | Les solutions sont instables. Préparer des solutions fraîches ou acheter des formats pré-emballés de petite taille. Reconditionner dès réception. | |
| Synonymes | Dinoprostone | Smiles | CCCCCC(C=CC1C(CC(=O)C1CC=CCCCC(=O)O)O)O | ||
|
In vitro |
DMSO
: 70 mg/mL
(198.59 mM)
Ethanol : 70 mg/mL Water : 2.5 mg/mL |
|
In vivo |
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Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)
Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)
Résultats du calcul :
Concentration de travail : mg/ml;
Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.
Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.
| In vitro |
La PGE2 agit via les récepteurs EP4 sur les ostéoclastes pendant la progression de l'arthrose et de la douleur liée à l'arthrose. |
|---|---|
| In vivo |
La PGE2 (0,3 μg/kg, i.p.) réduit significativement le nombre de macrophages péritonéaux subissant la phagocytose des microbilles de méthacrylate chez les rats. |
Références |
(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Sponsor/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| 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 |
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