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A-437203

Name: A-437203
Brand: TargetMol
SKU: T10213
Price: 91 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T10213Cas No. 220519-06-2

Alias Lu201640, ABT-925, A37203

A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ﬀ old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.

A-437203

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Purity: 98.80%

Catalog No. T10213Alias Lu201640, ABT-925, A37203Cas No. 220519-06-2

A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ﬀ old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$91	In Stock	In Stock
5 mg	$209	In Stock	In Stock
10 mg	$293	In Stock	In Stock
25 mg	$457	In Stock	In Stock
50 mg	$592	In Stock	In Stock
100 mg	$822	In Stock	In Stock
200 mg	$1,090	-	In Stock
1 mL x 10 mM (in DMSO)	$239	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.80%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	A-437203 (Lu201640) is A kind of based on 1 h - pyrimidin - 2 - one sca ﬀ old, selective, new powerful d3 receptor antagonist, on D2, d3, and D4 receptor, Ki value 71, respectively 1.6 and 6220 nM.
Targets&IC50	D2 receptor:71 nM (Ki), D4 receptor:6220 nM , D3 receptor:1.6 nM
In vitro	A-437203 is a high-affinity antagonist for D3 receptors with 44-fold selectivity over D2 receptors, demonstrating relatively high selectivity among dopamine receptor subtypes[1].
In vivo	A-437203 is initially tested alone in the 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 (F4, 45=1.12, p=0.359 for immobility, F4, 45=0.188, p=0.943 for climbing, and F4, 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].
Animal Research	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.).
Synonyms	Lu201640, ABT-925, A37203

Chemical Properties

Molecular Weight	456.53
Formula	C₂₀H₂₇F₃N₆OS
Cas No.	220519-06-2
Smiles	C(F)(F)(F)C1=CC(=NC(C(C)(C)C)=N1)N2CCN(CCCSC=3NC(=O)C=CN3)CC2
Relative Density.	1.35 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (131.43 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1904 mL	10.9522 mL	21.9044 mL	109.5218 mL
5 mM	0.4381 mL	2.1904 mL	4.3809 mL	21.9044 mL
10 mM	0.2190 mL	1.0952 mL	2.1904 mL	10.9522 mL
20 mM	0.1095 mL	0.5476 mL	1.0952 mL	5.4761 mL
50 mM	0.0438 mL	0.2190 mL	0.4381 mL	2.1904 mL
100 mM	0.0219 mL	0.1095 mL	0.2190 mL	1.0952 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc