Dopamine D2 receptor antagonist-1

Name: Dopamine D2 receptor antagonist-1
Brand: MedChemExpress
SKU: HY-129946
Rating: 4.5 (1 reviews)

Cat. No.: HY-129946 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.

For research use only. We do not sell to patients.

Dopamine D2 receptor antagonist-1 Chemical Structure

CAS No. : 1055411-77-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 176	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 176	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 160	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 660	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 930	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity^[1].

IC₅₀ & Target

D2R^[1]

Molecular Weight

259.37

Formula

C₁₄H₁₇N₃S

CAS No.

1055411-77-2

Appearance

Solid

Color

White to off-white

SMILES

C12=NC=NC(NC3CCC3)=C1C4=C(CCCC4)S2

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 : 250 mg/mL (963.87 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	3.8555 mL	19.2775 mL	38.5550 mL
5 mM	0.7711 mL	3.8555 mL	7.7110 mL
10 mM	0.3855 mL	1.9277 mL	3.8555 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)

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: ≥ 6.25 mg/mL (24.10 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 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)

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: 99.06%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (262 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[1]. Fyfe TJ, et al. Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D2 receptor. Eur J Med Chem. 2019 Apr 15;168:474-490. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8555 mL	19.2775 mL	38.5550 mL	96.3874 mL
	5 mM	0.7711 mL	3.8555 mL	7.7110 mL	19.2775 mL
	10 mM	0.3855 mL	1.9277 mL	3.8555 mL	9.6387 mL
	15 mM	0.2570 mL	1.2852 mL	2.5703 mL	6.4258 mL
	20 mM	0.1928 mL	0.9639 mL	1.9277 mL	4.8194 mL
	25 mM	0.1542 mL	0.7711 mL	1.5422 mL	3.8555 mL
	30 mM	0.1285 mL	0.6426 mL	1.2852 mL	3.2129 mL
	40 mM	0.0964 mL	0.4819 mL	0.9639 mL	2.4097 mL
	50 mM	0.0771 mL	0.3855 mL	0.7711 mL	1.9277 mL
	60 mM	0.0643 mL	0.3213 mL	0.6426 mL	1.6065 mL
	80 mM	0.0482 mL	0.2410 mL	0.4819 mL	1.2048 mL
	100 mM	0.0386 mL	0.1928 mL	0.3855 mL	0.9639 mL