Art. -Nr.: HY-U00185

A-437203

(Synonyms: Lu201640; A37203)

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A-437203 is a selective D₃ receptor antagonist with K_i of 71, 1.6, and 6220 nM for D₂, D₃, and D₄ receptors, respectively.

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Reinheit: 99.08%
CAS. Nr.: 220519-06-2
Formel: C₂₀H₂₇F₃N₆OS
Molecular Weight:456.53

Speicherung:

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

A-437203 Chemical Structure

CAS. Nr.: 220519-06-2

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

Biologische Aktivität

Beschreibung

A-437203 is a selective D₃ receptor antagonist with K_i of 71, 1.6, and 6220 nM for D₂, D₃, and D₄ receptors, respectively.

IC₅₀ & Target

Ki :71 nM (D₂ receptor), 1.6 nM (D₃ receptor), 6220 nM (D₄ receptor)^[1]

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

A-437203 is an antagonist with high affinity for D₃ receptors and relatively high selectivity compared to other dopamine receptor subtypes (44-fold selective for D₃ vs D₂)^[1].

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

In Vivo

A-437203, a selective D₃ receptor antagonist, is initially tested alone in rat forced swim test (FST). Doses of A-437203 evaluated are 0.52, 1.75, 5.24, and 17.46 μmol/kg i.p. Doses are chosen based on the selectivity of A-437203 for D₃ vs D₂ dopamine receptors and reports indicating that the effects of A-437203 at doses of 17.46 μmol/kg (10 mg/kg) or lower are clearly mediated by D₃ but not D₂ receptors, since higher doses of the compound such as 174.6 μmol/kg (100 mg/kg) are necessary to bind and block D₂ receptor from the irreversible inactivation induced by the alkylating agent EEDG. ANOVA revealed no significant difference between the treatments for any of the behaviors analyzed (F_{4, 45}=1.12, p=0.359 for immobility, F_{4, 45}=0.188, p=0.943 for climbing, and F_{4, 45}=1.634, p=0.182 for swimming). Based on these results, the dose of 17.46 μmol/kg i.p. of A-437203 is selected for further experiments^[1].

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

Chemical Information

CAS. Nr. 220519-06-2
Appearance Solid
Molecular Weight 456.53
Formel C₂₀H₂₇F₃N₆OS
Color Off-white to light yellow
SMILES

O=C1NC(SCCCN2CCN(C3=NC(C(C)(C)C)=NC(C(F)(F)F)=C3)CC2)=NC=C1
Synonyms

Lu201640; A37203
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 : ≥ 125 mg/mL (273.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.1904 mL

10.9522 mL

21.9044 mL

5 mM

0.4381 mL

2.1904 mL

4.3809 mL

10 mM

0.2190 mL

1.0952 mL

2.1904 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)}

Protokoll

Animal Administration^[1]

Rats^[1]
Male Sprague-Dawley rats weighing 250-350 g are used for these experiments. Haloperidol (0.27, 1.33, and 2.66 μmol/kg=0.1, 0.5, and 1.0 mg/kg i.p.), A-437203 (LU-201640) (0.52, 1.75, 5.24, and 17.46 μmol/kg=0.3, 1.0, 3.0, and 10.0 mg/kg i.p.), and L-745,870 (0.23, 1.15, 2.3, and 5.7 μmol/kg=0.1, 0.5, 1.0, and 2.5 mg/kg i.p.) are tested initially alone in order to determine effective dose ranges. In those experiments, haloperidol, A-437203, and L-745,870 are administered i.p. 24, 5, and 0.5 h before the test swim. In the subsequent antagonism experiments, Haloperidol (0.27 μmol/kg), A-437203 (17.46 μmol/kg) or L-745,870 (1.15 μmol/kg) are injected i.p. 15 min prior to each quinpirole injection (0.4 and 1.0 μmol/kg s.c.).

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Basso AM, et al. Antidepressant-like effect of D(2/3) receptor-, but not D(4) receptor-activation in the rat forced swim test. Neuropsychopharmacology. 2005 Jul;30(7):1257-68. [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	2.1904 mL	10.9522 mL	21.9044 mL	54.7609 mL
	5 mM	0.4381 mL	2.1904 mL	4.3809 mL	10.9522 mL
	10 mM	0.2190 mL	1.0952 mL	2.1904 mL	5.4761 mL
	15 mM	0.1460 mL	0.7301 mL	1.4603 mL	3.6507 mL
	20 mM	0.1095 mL	0.5476 mL	1.0952 mL	2.7380 mL
	25 mM	0.0876 mL	0.4381 mL	0.8762 mL	2.1904 mL
	30 mM	0.0730 mL	0.3651 mL	0.7301 mL	1.8254 mL
	40 mM	0.0548 mL	0.2738 mL	0.5476 mL	1.3690 mL
	50 mM	0.0438 mL	0.2190 mL	0.4381 mL	1.0952 mL
	60 mM	0.0365 mL	0.1825 mL	0.3651 mL	0.9127 mL
	80 mM	0.0274 mL	0.1369 mL	0.2738 mL	0.6845 mL
	100 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5476 mL

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A-437203

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Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-437203

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Neurotransmitter Receptor Compound Library

Neurodegenerative Disease-related Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Dopamine Receptor Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Dopamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

A-437203 Related Classifications

HY-U00185 Related Classifications