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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $34 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | $119 | In Stock | |
25 mg | $221 | In Stock | |
50 mg | $319 | In Stock | |
100 mg | $461 | In Stock | |
200 mg | $648 | In Stock | |
1 mL x 10 mM (in DMSO) | $80 | In Stock |
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 | D4.2 receptor:1.9 nM (Ki, cell free), D4.4 receptor:1.5 nM (Ki, cell free), D4.7 receptor:1.6 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]. |
Molecular Weight | 320.43 |
Formula | C20H24N4 |
Cas No. | 726174-00-1 |
Smiles | Cc1ccc(cc1C)N1CCN(Cc2nc3ccccc3[nH]2)CC1 |
Relative Density. | no data available |
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
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