Art. -Nr.: HY-175504

MLS6357

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MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.

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Reinheit: 99.57%
CAS. Nr.: 932544-59-7
Formel: C₁₈H₂₂ClN₃O₃S
Molecular Weight:395.90

Speicherung:

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

MLS6357 Chemical Structure

CAS. Nr.: 932544-59-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Dopamine D3 receptor

13 μM (IC₅₀)

Dopamine D1 receptor

Dopamine D2 receptor

Dopamine D4 receptor

Dopamine D5 receptor

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

MLS6357 fully antagonizes the attenuation of cAMP accumulation induced by an EC₈₀ concentration of Dopamine (HY-B0451) with an IC₅₀ of 4.5 μM and D3R-stimulation of ERK1/2 phosphorylation (pERK) with an IC₅₀ of 5.6 μM in HEK293 cells^[1].
MLS6357 exhibits moderate microsomal stability in human liver microsome (CL_int = 51 μL/min/mg; t_1/2 = 13.6 min)^[1].

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

Chemical Information

CAS. Nr. 932544-59-7
Appearance Solid
Molecular Weight 395.90
Formel C₁₈H₂₂ClN₃O₃S
Color White to off-white
SMILES

O=C(C1=C(NC(C)=C1S(NC2=CC(Cl)=C(C=C2)C)(=O)=O)C)N3CCCC3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (252.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5259 mL

12.6295 mL

25.2589 mL

5 mM

0.5052 mL

2.5259 mL

5.0518 mL

10 mM

0.2526 mL

1.2629 mL

2.5259 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 5 mg/mL (12.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (12.63 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Moritz AE, et al. Discovery, Characterization, and Optimization of a Novel Positive Allosteric Modulator-Antagonist of the D3 Dopamine Receptor. J Med Chem. 2025 Aug 14;68(15):16691-16749. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.5259 mL	12.6295 mL	25.2589 mL	63.1473 mL
	5 mM	0.5052 mL	2.5259 mL	5.0518 mL	12.6295 mL
	10 mM	0.2526 mL	1.2629 mL	2.5259 mL	6.3147 mL
	15 mM	0.1684 mL	0.8420 mL	1.6839 mL	4.2098 mL
	20 mM	0.1263 mL	0.6315 mL	1.2629 mL	3.1574 mL
	25 mM	0.1010 mL	0.5052 mL	1.0104 mL	2.5259 mL
	30 mM	0.0842 mL	0.4210 mL	0.8420 mL	2.1049 mL
	40 mM	0.0631 mL	0.3157 mL	0.6315 mL	1.5787 mL
	50 mM	0.0505 mL	0.2526 mL	0.5052 mL	1.2629 mL
	60 mM	0.0421 mL	0.2105 mL	0.4210 mL	1.0525 mL
	80 mM	0.0316 mL	0.1579 mL	0.3157 mL	0.7893 mL
	100 mM	0.0253 mL	0.1263 mL	0.2526 mL	0.6315 mL

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MLS6357

Cell Cycle/DNA Damage Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Neurotransmitter Receptor Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Dopamine Receptor Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MLS6357

Cell Cycle/DNA Damage Compound Library

GPCR/G Protein Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Anti-Aging Compound Library

Endoplasmic Reticulum Stress Compound Library

Neurotransmitter Receptor Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Dopamine Receptor Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MLS6357 Related Classifications

HY-175504 Related Classifications