2. GPCR/G Protein
  3. Adenosine Receptor
  4. DMPX

DMPX  (Synonyms: 3,7-Dimethyl-1-propargylxanthine)

Cat. No.: HY-W004425 Purity: 99.66%
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DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease.

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DMPX

DMPX Chemical Structure

CAS No. : 14114-46-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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10 mg In-stock
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DMPX Related Antibodies

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Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DMPX (3,7-Dimethyl-1-propargylxanthine) is a selective A2A adenosine receptor (A2A AR) antagonist that crosses the blood-brain barrier, with a Ki of 11 μM for rat A2 adenosine receptor and a Ki of 45 μM for rat A1 adenosine receptor. By blocking A2A receptors in specific brain regions, DMPX protects dopaminergic and GABAergic neurons from mitochondrial dysfunction. DMPX is applicable to research related to depression, Parkinson's disease and Huntington's disease[1][2][3].

IC50 & Target[2]

A2AR

11 μM (Ki)

A1AR

45 μM (Ki)

In Vivo

Co-administration of DMPX (3 mg/kg; i.p.; single dose) with Agomelatine (HY-17038) or Tianeptine (HY-90003) produces synergistic antidepressant-like effects in mouse behavioral despair tests. These effects correlate with increased brain concentrations of the co-administered antidepressants, without altering spontaneous locomotor activity[1].
DMPX (0.032-10 mg/kg; 9.9 μmol/kg; i.p.; single administration) is a potent and selective in vivo A2 adenosine receptor antagonist. It is 57 times more potent at blocking NECA-induced hypothermia than CHA (HY-18939)-induced hypothermia, and 11 times more potent at blocking NECA (HY-103173)-induced motor inhibition than CHA-induced motor inhibition. In addition, its intrinsic motor stimulant potency (ED50 = 9.9 μmoL/kg) is slightly higher than that of caffeine[2].
DMPX (5 mg/kg; i.p.; single administration) significantly attenuates the malonate-induced depletion of striatal dopamine and tyrosine hydroxylase (TH). In rats, DMPX also completely blocks malonate-induced striatal GABA loss[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Albino Swiss (male, adult, 25-30 g)[1]
Dosage: 3 mg/kg
Administration: i.p.; single dose (30 minutes prior to tests/decapitation)
Result: Significantly reduced the immobility time of mice in the forced swimming test and the tail suspension test, and produced an antidepressant-like synergistic effect.
Animal Model: DBA/2 (10-week-old, male, inbred)[2]
Dosage: 0.032, 0.1, 0.32, 1.0, 3.2, 10 mg/kg (blockade of hypothermia/locomotor depression); 9.9 μmol/kg (intrinsic locomotor stimulation)
Administration: i.p.; single dose; 15 minutes prior to agonist administration (blockade assays); i.p.; single dose (intrinsic stimulation assay)
Result: Antagonized NECA-induced hypothermia and motor inhibition.
Animal Model: Swiss-Webster (male, 30-35 gm) and Sprague-Dawley (male, 300-375 gm, intrastriatal malonate infusion induced)[3]
Dosage: 5 mg/kg
Administration: i.p.; single dose; 30 min prior to malonate infusion
Result: Significantly alleviated the depletion of dopamine and TH in the striatum caused by succinic acid.
Completely blocked the loss of GABA in the striatum caused by succinic acid in rats.
Molecular Weight

218.21

Formula

C10H10N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N(C)C(N1CC#C)=O)N=CN2C
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 : 40 mg/mL (183.31 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 4.5827 mL 22.9137 mL 45.8274 mL
5 mM 0.9165 mL 4.5827 mL 9.1655 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4 mg/mL (18.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (40.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 4 mg/mL (18.33 mM); Clear solution

    This protocol yields a clear solution of ≥ 4 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 (40.0 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

Animal weight
(per animal)

g

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
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 4.5827 mL 22.9137 mL 45.8274 mL 114.5685 mL
5 mM 0.9165 mL 4.5827 mL 9.1655 mL 22.9137 mL
10 mM 0.4583 mL 2.2914 mL 4.5827 mL 11.4569 mL
15 mM 0.3055 mL 1.5276 mL 3.0552 mL 7.6379 mL
20 mM 0.2291 mL 1.1457 mL 2.2914 mL 5.7284 mL
25 mM 0.1833 mL 0.9165 mL 1.8331 mL 4.5827 mL
30 mM 0.1528 mL 0.7638 mL 1.5276 mL 3.8190 mL
40 mM 0.1146 mL 0.5728 mL 1.1457 mL 2.8642 mL
50 mM 0.0917 mL 0.4583 mL 0.9165 mL 2.2914 mL
60 mM 0.0764 mL 0.3819 mL 0.7638 mL 1.9095 mL
80 mM 0.0573 mL 0.2864 mL 0.5728 mL 1.4321 mL
100 mM 0.0458 mL 0.2291 mL 0.4583 mL 1.1457 mL
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DMPX Related Classifications

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:

DMPX14114-46-63,7-Dimethyl-1-propargylxanthineAdenosine ReceptorP1 receptorblood-brain barriermouse forced swim testsrat A2 adenosine receptortail suspension testsdepressionadenosine A2? receptorParkinson’s diseaserat A1 adenosine receptortianeptineagomelatineInhibitorinhibitorinhibit

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