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DPA-714 (DPA714; DPA 714) is a novel and selective ligand for translocator protein (TSPO) with the potential to be used as a PET tracer binding the TSPO receptor that is over-expressed in myeloid cells.
| ln Vivo |
[18F]DPA-714 binding is dramatically elevated in vivo due to AD-like pathology and age in APPswe×PS1Δe9 mice.
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| References |
[1]. James ML, et al. DPA-714, a new translocator protein-specific ligand: synthesis, radiofluorination, and pharmacologic characterization. J Nucl Med. 2008 May;49(5):814-22.
[2]. Harhausen D, et al. Specific imaging of inflammation with the 18 kDa translocator protein ligand DPA-714 in animal models of epilepsy and stroke. PLoS One. 2013 Aug 2;8(8):e69529. |
| Molecular Formula |
C22H27FN4O2
|
|---|---|
| Molecular Weight |
398.48
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| Exact Mass |
398.211
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| CAS # |
958233-07-3
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| PubChem CID |
24895172
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Index of Refraction |
1.581
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| LogP |
2.86
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
525
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CC1=C2N=C(C)C=C(N2N=C1C1C=CC(OCCF)=CC=1)C)N(CC)CC
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| InChi Key |
FLZZFWBNYJNHMY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H27FN4O2/c1-5-26(6-2)20(28)14-19-21(17-7-9-18(10-8-17)29-12-11-23)25-27-16(4)13-15(3)24-22(19)27/h7-10,13H,5-6,11-12,14H2,1-4H3
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| Chemical Name |
N,N-diethyl-2-(2-(4-(2-fluoroethoxy)phenyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)acetamide
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| Synonyms |
DPA714DPA-714 DPA 714J2.865.885K
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~41.67 mg/mL (~104.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5095 mL | 12.5477 mL | 25.0954 mL | |
| 5 mM | 0.5019 mL | 2.5095 mL | 5.0191 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5095 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06289582 | NOT YET RECRUITING | Drug: [F-18]DPA714 administration IV | Parkinson Disease | University of Alabama at Birmingham | 2024-06 | Early Phase 1 |
| NCT05672082 | WITHDRAWN | Drug: [18F]DPA-714 | Glioma | Center Eugene Marquis | 2023-10-01 | Not Applicable |
| NCT03759522 | RECRUITING | Drug: DPA-714 PET/MRI | Chronic Fatigue Syndrome Fibromyalgia Healthy Multiple Sclerosis |
University of Alabama at Birmingham | 2019-02-03 | Phase 1 |
| NCT04320030 | COMPLETED | Drug: [18F]-DPA-714 PET/CT scan | Triple Negative Breast Cancer | Institut Cancerologie de l'Ouest | 2020-06-11 | Phase 2 |
| NCT03457493 | RECRUITING | Drug: DPA-714-PET/MRI Drug: 5-year Follow-up DPA-714-PET/MRI Drug: DPA-714 Metabolite Analysis |
Parkinson Disease | University of Alabama at Birmingham | 2018-03-22 | Phase 1 Phase 2 |
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