2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. A-381393

A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM).

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A-381393 Chemical Structure

A-381393 Chemical Structure

CAS No. : 726174-00-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 In-stock
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Solid
1 mg USD 71 In-stock
5 mg USD 150 In-stock
10 mg USD 250 In-stock
25 mg USD 450 In-stock
50 mg USD 650 In-stock
100 mg USD 950 In-stock
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

A-381393 Related Antibodies

Top Publications Citing Use of Products

View All Dopamine Receptor Isoform Specific Products:

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM)[1].

IC50 & Target

Ki: 1.5 nM (D4.4 receptor), 1.9 nM (D4.2 receptor), 1.6 nM (D4.7 receptor)[1]
In Vitro

A-381393 exhibits weak affinity at 5-HT1A, Sigma 2, Adenoceptor α1A, Adenoceptor α2C, Histamine H1, with Kis of 1365, 8600, 2044, 1912 and 2962 nM, respectively[1].

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

A-381393 Related Antibodies
Molecular Weight

320.43

Formula

C20H24N4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC=C(C=C1C)N2CCN(CC2)CC3=NC4=CC=CC=C4N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 51.67 mg/mL (161.25 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 3.1208 mL 15.6040 mL 31.2081 mL
5 mM 0.6242 mL 3.1208 mL 6.2416 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.58 mg/mL (8.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.58 mg/mL (8.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.58 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1208 mL 15.6040 mL 31.2081 mL 78.0202 mL
5 mM 0.6242 mL 3.1208 mL 6.2416 mL 15.6040 mL
10 mM 0.3121 mL 1.5604 mL 3.1208 mL 7.8020 mL
15 mM 0.2081 mL 1.0403 mL 2.0805 mL 5.2013 mL
20 mM 0.1560 mL 0.7802 mL 1.5604 mL 3.9010 mL
25 mM 0.1248 mL 0.6242 mL 1.2483 mL 3.1208 mL
30 mM 0.1040 mL 0.5201 mL 1.0403 mL 2.6007 mL
40 mM 0.0780 mL 0.3901 mL 0.7802 mL 1.9505 mL
50 mM 0.0624 mL 0.3121 mL 0.6242 mL 1.5604 mL
60 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3003 mL
80 mM 0.0390 mL 0.1951 mL 0.3901 mL 0.9753 mL
100 mM 0.0312 mL 0.1560 mL 0.3121 mL 0.7802 mL
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A-381393 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:

A-381393726174-00-1A381393A 381393Dopamine ReceptorInhibitorinhibitorinhibit

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