DPA-713
Based on 1 Customer Validation
DPA-713 is a blood-brain barrier-permeable, specific translocator protein (TSPO) ligand. DPA-713 binds exclusively to TSPO without interacting with central benzodiazepine receptors; its binding can be competitively displaced by excess unlabeled TSPO ligands. After 11C labeling, DPA-713 enables sensitive quantitative analysis of TSPO expression associated with microglial activation, allowing differentiation between normal and pathological brain tissues. DPA-713 can be used in studies related to neuroinflammation, neurodegenerative diseases, and recently onset schizophrenia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.86%
- CAS. Nr.: 386297-97-8
- Formel: C21H26N4O2
- Molecular Weight:366.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
100 μM
Compound: DPA-713
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Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
Cytotoxicity against HEK293T cells expressing human wild type TSPO assessed as decrease in cell viability after 48 hrs by CellTiter blue assay
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[PMID: 30108706] |
| HEK-293T | IC50 |
>100 μM
Compound: DPA-713
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Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
Antiproliferative activity against HEK293T cells expressing human TSPO A147T mutant after 48 hrs by BrdU incorporation assay
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[PMID: 30108706] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 386297-97-8
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Appearance Solid
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Molecular Weight 366.47
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Formel C21H26N4O2
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Color White to off-white
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SMILES
O=C(N(CC)CC)CC=1C(=NN2C1N=C(C=C2C)C)C=3C=CC(OC)=CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (272.87 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.64 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Boutin H, et al. 11C-DPA-713: a novel peripheral benzodiazepine receptor PET ligand for in vivo imaging of neuroinflammation. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2007 Apr;48(4):573-81. [Content Brief]
[2]. Endres CJ, et al. Initial evaluation of 11C-DPA-713, a novel TSPO PET ligand, in humans. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2009 Aug;50(8):1276-82. [Content Brief]
[3]. Coughlin JM, et al. In vivo markers of inflammatory response in recent-onset schizophrenia: a combined study using [(11)C]DPA-713 PET and analysis of CSF and plasma. Translational psychiatry. 2016 Apr 12;6(4):e777. [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. 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 | 2.7287 mL | 13.6437 mL | 27.2874 mL | 68.2184 mL |
| 5 mM | 0.5457 mL | 2.7287 mL | 5.4575 mL | 13.6437 mL | |
| 10 mM | 0.2729 mL | 1.3644 mL | 2.7287 mL | 6.8218 mL | |
| 15 mM | 0.1819 mL | 0.9096 mL | 1.8192 mL | 4.5479 mL | |
| 20 mM | 0.1364 mL | 0.6822 mL | 1.3644 mL | 3.4109 mL | |
| 25 mM | 0.1091 mL | 0.5457 mL | 1.0915 mL | 2.7287 mL | |
| 30 mM | 0.0910 mL | 0.4548 mL | 0.9096 mL | 2.2739 mL | |
| 40 mM | 0.0682 mL | 0.3411 mL | 0.6822 mL | 1.7055 mL | |
| 50 mM | 0.0546 mL | 0.2729 mL | 0.5457 mL | 1.3644 mL | |
| 60 mM | 0.0455 mL | 0.2274 mL | 0.4548 mL | 1.1370 mL | |
| 80 mM | 0.0341 mL | 0.1705 mL | 0.3411 mL | 0.8527 mL | |
| 100 mM | 0.0273 mL | 0.1364 mL | 0.2729 mL | 0.6822 mL |
DPA-713 Related Classifications
HY-W667746 Related Classifications
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Keywords
- DPA-713
- 386297-97-8
- DPA713
- DPA 713
- TSPO
- Radionuclide-Drug Conjugates (RDCs)
- recent-onset schizophrenia
- blood-brain barrier
- neurodegenerative diseases
- neuroinflammation
- translocator protein (TSPO)
- central benzodiazepine receptors
- rat brain tissue
- baboons
- TSPO rs6971 genotype
- microglial activation
- Inhibitor
- inhibitor
- inhibit