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Réf. Catalogue: S1985
| Lignées cellulaires | Type d'essai | Concentration | Temps d'incubation | Formulation | Description de l'activité | PMID |
|---|---|---|---|---|---|---|
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y114A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0301μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged wild type 4 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0631μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 2, EC50=0.085μM. | 11985476 | |||
| 1321N1 | Function assay | Agonist activity at human P2Y2 receptor expressed in human 1321N1 cells coexpressing phospholipase C-activating G protein assessed as inositol phosphate production by scintillation proximity assay, EC50=0.085μM. | 19419868 | |||
| 1321N1 | Function assay | Agonist activity at human recombinant P2Y2 receptor expressed in 1321N1 cells assessed as stimulation of phospholipase C, EC50=0.085μM. | 17302398 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged wild type 3 human P2Y2 receptor expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.0958μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R194H mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.111μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y198A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.12μM. | 19419204 | |||
| MDCK | Function assay | 10 uM | Induction of intracellular calcium level in MDCK cells assessed as net peak value at 10 uM by Fura-2 in calcium free medium, Activity=0.132μM. | 23163425 | ||
| 1321N1 | Function assay | 30 mins | Agonist activity at GFP tagged-human P2Y1 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=0.15μM. | 21090681 | ||
| NG108-15 | Function assay | Agonist activity at P2Y2 receptor in NG108-15 cells (unknown origin), EC50=0.18μM. | 29254895 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.183μM. | 19419204 | |||
| HEK293 | Function assay | Agonist activity at P2Y1 receptor expressed in human HEK293 cells, EC50=0.2μM. | 20175517 | |||
| HEK293 | Function assay | Agonist activity at rat P2Y1R expressed in HEK293 cells assessed as release of intracellular calcium by fluorescence based assay, EC50=0.2μM. | 22873688 | |||
| CF/T43 | Function assay | Agonist activity at P2Y2 receptor in human CF/T43 cells, EC50=0.2μM. | 29254895 | |||
| BEA | Function assay | Agonist activity at P2Y2 receptor in BEA cells (unknown origin), EC50=0.2μM. | 29254895 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R180A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.237μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R177A_R180A double mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.239μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor Y118A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=0.299μM. | 19419204 | |||
| HEK 293 | Function assay | Concentration required for calcium mobilization at rat purinergic 2Y1 receptor expressed in HEK 293 cells, EC50=0.59μM. | 15317453 | |||
| 1321N1 | Function assay | Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells, Kb=0.708μM. | 17302398 | |||
| 1321N1 | Function assay | Agonist activity at human GFP-tagged P2Y1R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=0.85μM. | 23751098 | |||
| 1321N1 | Function assay | 30 mins | Agonist activity at human P2Y1 receptor expressed in human 1321N1 cells assessed as increase of intracellular calcium level after 30 mins using fura-2 AM by fluorescence assay, EC50=0.85μM. | 24846781 | ||
| 1321N1 | Function assay | Agonist activity at GFP-tagged human P2Y1R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=0.85μM. | 26447940 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor C278S mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=1μM. | 19419204 | |||
| 1321N1 | Function assay | 30 mins | Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method, EC50=1μM. | 23075067 | ||
| Sf9 | Function assay | Binding affinity to wild type 6XHis-tagged human JAK2 JH2 domain (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. | 32329617 | |||
| Sf9 | Function assay | Binding affinity to 6XHis-tagged human JAK2 JH2 domain V617F mutant (513 to 827 residues) expressed in baculovirus infected Sf9 cells by MANT-ATP binding assay, Kd=1.3μM. | 32329617 | |||
| 1321N1 | Function assay | Accumulation of inositol phosphate in 1321N1 astrocytoma cells expressing human P2Y1 purinoceptor, EC50=1.5μM. | 11985476 | |||
| Sf9 | Function assay | Binding affinity to recombinant human biotinylated N-terminal GST-tagged autophosphorylated TAK1 (1 to 303 residues) fused with TAB1 (437 to 504 residues) expressed in baculovirus infected sf9 cells by SPR assay, Kd=2.8μM. | 28109791 | |||
| 1321N1 | Function assay | 30 mins | Agonist activity at GFP tagged-human P2Y11 receptor expressed in human 1321N1 cells assessed as elevation in calcium level after 30 mins by fluorescence spectrophotometric analysis, EC50=3.3μM. | 21090681 | ||
| 1321N1 | Function assay | Agonist activity at human GFP-tagged P2Y11R transfected in human 1321N1 cells assessed as induction of intracellular calcium mobilization by fluorescence assay, EC50=6.7μM. | 23751098 | |||
| 1321N1 | Function assay | Agonist activity at GFP-tagged human P2Y11R transfected in human 1321N1 cells assessed as increase in intracellular Ca2+ level by fura 2/AM probe-based fluorescence assay, EC50=6.7μM. | 26447940 | |||
| 1321N1 | Function assay | Agonist activity at N-terminal HA epitope-tagged human P2Y2 receptor R272A mutant expressed in human 1321N1 cells assessed as increase in intracellular calcium level, EC50=11.7μM. | 19419204 | |||
| 1321N1 | Function assay | Agonist activity by measuring inositol phosphate accumulation in 1321N1 human astrocytoma cells stably expressing human P2Y purinoceptor 11, EC50=17.3μM. | 11985476 | |||
| 1321N1 | Function assay | Antagonistic activity at human recombinant P2Y4 receptor expressed in 1321N1 cells | 17302398 | |||
| MDCK | Function assay | 10 uM | Induction of intracellular calcium level in MDCK cells at 10 uM by Fura-2 in calcium free medium in presence of 10 uM U73343 inactive analogue of U73122 phospholipase C inhibitor | 23163425 | ||
| THLP1 | Function assay | Agonist activity at NLRP3 in human THLP1-null cells assessed as induction of LPS-induced IL-1beta secretion by HEK-Blue reporter cell based assay | 28829599 | |||
| HEK293 | Function assay | 1 uM | Agonist activity at ALX/FPR2 (unknown origin) expressed in HEK293 cells co-expressing Galphaq assessed as induction of intracellular calcium accumulation at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay | 30419493 | ||
| HEK293 | Function assay | 1 uM | Induction of intracellular calcium accumulation in HEK293 cells at 1 uM by Fluo-4 dye based fluorescence spectrophotometric assay | 30419493 | ||
| BL21(DE3) | Function assay | Activity of Bacillus subtilis N-terminal His-tagged ANT(6) expressed in Escherichia coli BL21(DE3) cells assessed as adenylated product by Michaelis-Menten kinetics | ChEMBL | |||
| Cliquez pour voir plus de données expérimentales sur la lignée cellulaire | ||||||
| Poids moléculaire | 551.14 | Formule | C10H14N5O13P3.2Na |
Stockage (À compter de la date de réception) | |
|---|---|---|---|---|---|
| N° CAS | 987-65-5 | Télécharger le SDF | Stockage des solutions mères |
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| Synonymes | Adenosine-Triphosphate disodium, Adenosine 5'-triphosphate | Smiles | C1=NC(=C2C(=N1)N(C=N2)C3C(C(C(O3)COP(=O)(O)OP(=O)([O-])OP(=O)(O)[O-])O)O)N.[Na+].[Na+] | ||
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In vitro |
Water : 100 mg/mL
DMSO
: Insoluble
Ethanol : Insoluble |
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In vivo |
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Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)
Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.
Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.
Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.
| In vitro |
La libération d'ATP et la rétroaction autocrine via les récepteurs P2Y2 et A3 assurent l'amplification du signal, contrôlant la détection du gradient et la migration des neutrophiles. L'ATP entraîne la production d'espèces réactives de l'oxygène (ROS), ce qui stimule la voie de la phosphatidylinositol 3-kinase (PI3K) et l'activation subséquente d'Akt et d'ERK1/2. La production de ROS dépendante de l'ATP et l'activation de la PI3K stimulent également la transcription des gènes nécessaires à une réponse au stress oxydatif. La PI3K dépendante des ROS et médiatisée par l'ATP est nécessaire à l'activation de la caspase-1 et à la sécrétion d'IL-1beta et d'IL-18. L'ATP stimule puissamment la libération de TNF-alpha, résultant de l'expression de l'ARNm du TNF-alpha dans les microglies cérébrales de rat cultivées. La libération de TNF-alpha induite par l'ATP est dépendante du Ca(2+), et un afflux soutenu de Ca(2+) était corrélé à la libération de TNF-alpha dans les microglies stimulées par l'ATP. La libération de TNF-alpha induite par l'ATP est inhibée par le PD 098059, un inhibiteur de la protéine kinase régulée par le signal extracellulaire (ERK) kinase 1 (MEK1), qui active l'ERK, et également par le SB 203580, un inhibiteur de la protéine kinase activée par les mitogènes p38. L'ATP active rapidement l'ERK et la p38 même en l'absence de Ca(2+) extracellulaire. La cytotoxicité induite par l'ATP est médiatisée par des altérations classiques de l'apoptose, y compris le blebbing membranaire, la condensation nucléaire et la fragmentation de l'ADN. L'ATP, mais pas les autres nucléotides, conduit à l'activation puissante et sélective de NF-κB dans les cellules microgliales via une voie médiatisée par le récepteur P2Z. |
|---|---|
| In vivo |
L'ATP régule la dynamique des branches microgliales dans le cerveau de souris intact, et sa libération du tissu endommagé et des astrocytes environnants médie une réponse microgliale rapide à la blessure. |
Références |
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(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)
| Numéro NCT | Recrutement | Conditions | Promoteur/Collaborateurs | Date de début | Phases |
|---|---|---|---|---|---|
| NCT04760860 | Not yet recruiting | Dementia With Lewy Bodies |
Qiang Zhang|University of Iowa |
October 2024 | Phase 1|Phase 2 |
| NCT05590195 | Not yet recruiting | Bacterial Vaginosis|Bacterial Infections|Bacterial Vaginosis | Vaginal | Microbiology|Vaginal Infection |
Jeremy Burton|Deerland Enzymes|Lawson Health Research Institute|St. Joseph''s Health Care London |
May 1 2024 | Phase 3 |
| NCT06167512 | Not yet recruiting | Multi-organ Failure After Severe Trauma |
Assistance Publique - Hôpitaux de Paris |
April 1 2024 | -- |