CP 226269
Based on 1 Customer Validation
CP 226269 is a potent dopamine D4 receptor agonist that induces calcium flux with EC50 of 32 nM. CP 226269 stimulates phospholipid methylation (PLM) in SK-N-MC neuroblastoma cells with an EC50 of 2.9 nM. CP 226269 can be used in the research of schizophrenia and other related diseases.
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- Pureza : 99.65%
- No. CAS: 220941-93-5
- Fòrmula: C18H19FN4
- Peso molecular:310.37
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
D4 Receptor |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
22 nM
Compound: 8, (CP-226269)
|
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay
|
[PMID: 15239663] |
| HEK293 | EC50 |
32 nM
Compound: 8, (CP-226269)
|
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay
|
[PMID: 15239663] |
| HEK293 | EC50 |
36 nM
Compound: 8, (CP-226269)
|
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay
|
[PMID: 15239663] |
| HEK293 | EC50 |
527 nM
Compound: 8, (CP-226269)
|
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay
|
[PMID: 15239663] |
| HEK293 | EC50 |
55 nM
Compound: 8, (CP-226269)
|
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay
|
[PMID: 15239663] |
In Vitro
CP 226269 (30 minutes) stimulates phospholipid methylation (PLM) in SK-N-MC neuroblastoma cells, with a half-maximal effective concentration of 2.9 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats[3]
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Dosage:10, 30 mg/kg
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Administration:i.p., once
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Result:Exacerbated motor hyperactivity.
Chemical Information
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No. CAS 220941-93-5
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Appearance Solid
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Peso molecular 310.37
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Fòrmula C18H19FN4
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Color Light yellow to yellow
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SMILES
FC1=CC2=C(C=C1)NC(CN3CCN(CC3)C4=NC=CC=C4)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 125 mg/mL (402.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sharma A, et al. D4 dopamine receptor-mediated phospholipid methylation and its implications for mental illnesses such as schizophrenia. Mol Psychiatry. 1999 May;4(3):235-46. [Content Brief]
[2]. Robert B Moreland, et al. Comparative pharmacology of human dopamine D(2)-like receptor stable cell lines coupled to calcium flux through Galpha(qo5). Biochem Pharmacol. 2004 Aug 15;68(4):761-72. [Content Brief]
[3]. Zhang K, et al. Role of dopamine D(4) receptors in motor hyperactivity induced by neonatal 6-hydroxydopamine lesions in rats. Neuropsychopharmacology. 2001 Nov;25(5):624-32. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2220 mL | 16.1098 mL | 32.2196 mL | 80.5490 mL |
| 5 mM | 0.6444 mL | 3.2220 mL | 6.4439 mL | 16.1098 mL | |
| 10 mM | 0.3222 mL | 1.6110 mL | 3.2220 mL | 8.0549 mL | |
| 15 mM | 0.2148 mL | 1.0740 mL | 2.1480 mL | 5.3699 mL | |
| 20 mM | 0.1611 mL | 0.8055 mL | 1.6110 mL | 4.0275 mL | |
| 25 mM | 0.1289 mL | 0.6444 mL | 1.2888 mL | 3.2220 mL | |
| 30 mM | 0.1074 mL | 0.5370 mL | 1.0740 mL | 2.6850 mL | |
| 40 mM | 0.0805 mL | 0.4027 mL | 0.8055 mL | 2.0137 mL | |
| 50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6110 mL | |
| 60 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3425 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0069 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8055 mL |