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A-381393
🥰Excellent
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).
A-381393
🥰Excellent
Purity: 99.92%
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).
| 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 |
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Purity:99.92%
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.Product Introduction
Bioactivity
Chemical Properties
| 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 & 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 | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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