Tosylate-DPA-714
Based on 1 Customer Validation
Tosylate-DPA-714 is a GMP-grade precursor for the radiosynthesis of DPA-714 (HY-122607). It crosses the blood-brain barrier and exhibits steroidogenic activity. DPA-714 is a specific ligand for the 18 kDa translocator protein (TSPO) with a Ki of 7.0 nM. Tosylate-DPA-714 is safe and does not bind to central benzodiazepine receptors (benzodiazepine receptor). As a radiolabeling precursor, Tosylate-DPA-714 reacts with 18F via nucleophilic aliphatic substitution to form 18F-DPA-714, enabling specific targeted binding to TSPO. 18F-DPA-714 accurately reflects the level of neuroinflammation mediated by microglial activation, and is used for PET molecular imaging of neurological diseases such as Alzheimer's disease and multiple sclerosis.
For research use only. We do not sell to patients.
- Purity: 98.78%
- CAS No.: 958233-17-5
- Formula: C29H34N4O5S
- Molecular Weight:550.67
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Neuronal Signaling Compound Library
HY-L013
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CNS-Penetrant Compound Library
HY-L028
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Neurodegenerative Disease-related Compound Library
HY-L086
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
Tosylate-DPA-714 (40 μM; 2 h) increases pregnenolone synthesis by 80% relative to baseline in steroidogenic assays of rat C6 glioma cells, and its steroidogenic activity is significantly stronger than that of PK11195 (HY-19567)[1].
Tosylate-DPA-714 (0.1 nM-10 μM; 90 min) exhibits a Ki value of 7.0 nM for TSPO in a rat renal cell membrane TSPO binding assay, with high TSPO selectivity and no binding to central benzodiazepine receptors[1].
In lipophilicity assays, Tosylate-DPA-714 has a measured logD value of 2.44, with lower lipophilicity than the classic TSPO probe PK11195[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
18F-labeled Tosylate-DPA-714 (100 MBq; intravenous injection; single administration; 60 min dynamic scan) rapidly penetrates the blood-brain barrier and remains stably retained in normal male baboon models, with specific and reversible binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (300-320 g) with unilateral quinolinic acid striatal lesion[1]
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Dosage:20-37 MBq; pretreatment with PK11195 (5 mg/kg), DPA-714 (1 mg/kg) or DPA-713 (1 mg/kg)
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Administration:Single dose via penile vein injection; detected at 60 min post-administration
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Result:Showed an 8-fold higher uptake in the ipsilateral striatum than the contralateral side, and the specific uptake was completely inhibited by TSPO ligands.
Chemical Information
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CAS No. 958233-17-5
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Appearance Solid
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Molecular Weight 550.67
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Formula C29H34N4O5S
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Color Off-white to light yellow
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SMILES
O=C(CC1=C(N=C(C)C=C2C)N2N=C1C3=CC=C(OCCOS(=O)(C4=CC=C(C)C=C4)=O)C=C3)N(CC)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (181.60 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
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 | 1.8160 mL | 9.0798 mL | 18.1597 mL | 45.3992 mL |
| 5 mM | 0.3632 mL | 1.8160 mL | 3.6319 mL | 9.0798 mL | |
| 10 mM | 0.1816 mL | 0.9080 mL | 1.8160 mL | 4.5399 mL | |
| 15 mM | 0.1211 mL | 0.6053 mL | 1.2106 mL | 3.0266 mL | |
| 20 mM | 0.0908 mL | 0.4540 mL | 0.9080 mL | 2.2700 mL | |
| 25 mM | 0.0726 mL | 0.3632 mL | 0.7264 mL | 1.8160 mL | |
| 30 mM | 0.0605 mL | 0.3027 mL | 0.6053 mL | 1.5133 mL | |
| 40 mM | 0.0454 mL | 0.2270 mL | 0.4540 mL | 1.1350 mL | |
| 50 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.9080 mL | |
| 60 mM | 0.0303 mL | 0.1513 mL | 0.3027 mL | 0.7567 mL | |
| 80 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5675 mL | |
| 100 mM | 0.0182 mL | 0.0908 mL | 0.1816 mL | 0.4540 mL |
Tosylate-DPA-714 Related Classifications
HY-400882 Related Classifications
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