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A-381393

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Purity:99.92%

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COA HNMR HPLC

A-381393

Catalog No. T5397Cas No. 726174-00-1

A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

Pack Size	Price	Availability
1 mg	$56	In Stock
2 mg	$79	In Stock
5 mg	$122	In Stock
10 mg	$198	In Stock
25 mg	$369	In Stock
50 mg	$531	In Stock
100 mg	$768	In Stock
1 mL x 10 mM (in DMSO)	$133	In Stock

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Product Introduction

Bioactivity

Description	A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9/1.5/1.6 nM for human dopamine D4.2/D4.4/D4.7 receptor).
Targets&IC50	D4.7 receptor:1.6 nM (Ki, cell free), D4.4 receptor:1.5 nM (Ki, cell free), D4.2 receptor:1.9 nM (Ki, cell free)
In vitro	A-381393 potently bound to the membrane from cells expressing recombinant human dopamine D4.4 receptor (Ki=1.5 nM), which was 20-fold higher than that of clozapine (Ki=30.4 nM). A-381393 exhibited highly selective binding for the dopamine D4.4 receptor (>2700-fold) when compared to D1, D2, D3, and D5 dopamine receptors. A-381393 potently inhibited the functional activity of agonist-induced GTP-gamma-S binding assay and 1 microM dopamine-induced-Ca2+ flux in human dopamine D4.4 receptor-expressing cells, but not in human dopamine D2L or D3 receptor cells [1]. A-381393 blocked both c-Fos expression and ERK1/2 phosphorylation produced by PD168077. Treatment with A-381393 alone significantly reduced the amount of Fos immunoreactivity as compared to basal expression observed in vehicle-treated controls [2].

Chemical Properties

Molecular Weight	320.43
Formula	C20H24N4
Cas No.	726174-00-1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 50 mg/mL (156.04 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1208 mL	15.6040 mL	31.2081 mL	156.0403 mL
5 mM	0.6242 mL	3.1208 mL	6.2416 mL	31.2081 mL
10 mM	0.3121 mL	1.5604 mL	3.1208 mL	15.6040 mL
20 mM	0.1560 mL	0.7802 mL	1.5604 mL	7.8020 mL
50 mM	0.0624 mL	0.3121 mL	0.6242 mL	3.1208 mL
100 mM	0.0312 mL	0.1560 mL	0.3121 mL	1.5604 mL

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In Vivo Formulation Calculator (Clear solution)

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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