Tosylate-DPA-714

Cat. No.: HY-400882 Purity: 98.78%: Data Sheet
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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 K_i 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.

Tosylate-DPA-714 Chemical Structure

CAS No. : 958233-17-5

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Description

In Vitro

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 K_i 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.

In Vivo

¹⁸F-labeled Tosylate-DPA-714 (20-37 MBq; single dose via penile vein injection; detected at 60 min post-administration) shows significantly higher uptake in the lesioned cerebral hemisphere than in the contralateral hemisphere in male Wistar rats with unilateral striatal injury induced by quinolinic acid, and this uptake can be completely blocked by TSPO ligands^[1].
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.

Animal Model:	Male Wistar rats (300-320 g) with unilateral quinolinic acid striatal lesion^[1]
Dosage:	20-37 MBq; pretreatment with PK11195 (5 mg/kg), DPA-714 (1 mg/kg) or DPA-713 (1 mg/kg)
Administration:	Single dose via penile vein injection; detected at 60 min post-administration
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.

Molecular Weight

550.67

Formula

C₂₉H₃₄N₄O₅S

CAS No.

958233-17-5

Appearance

Solid

Color

Off-white to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8160 mL	9.0798 mL	18.1597 mL
5 mM	0.3632 mL	1.8160 mL	3.6319 mL
10 mM	0.1816 mL	0.9080 mL	1.8160 mL

View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (9.08 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 98.78%

Select Batch:

Data Sheet (276 KB) SDS (396 KB)

COA (251 KB)

Handling Instructions (2659 KB)

References

[1]. James M L, et al. DPA-714, a new translocator protein–specific ligand: synthesis, radiofluorination, and pharmacologic characterization[J]. Journal of Nuclear Medicine, 2008, 49(5): 814-822.

[2]. Cybulska KA, et al. Optimised GMP-compliant production of [¹⁸F]DPA-714 on the Trasis AllinOne module. EJNMMI Radiopharm Chem. 2021;6(1):20. Published 2021 May 26.

Complete Stock Solution Preparation Table

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

Neurological Disease Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tosylate-DPA-714958233-17-5Drug IntermediateDrug DerivativeTSPODrug IintermediateDrug derivativeTranslocator Proteintranslocator protein 18 kDaInhibitorinhibitorinhibit

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Tosylate-DPA-714

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