Powder: -20°C for 3 years | In solvent: -80°C for 1 year
lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 11,000 | |||
10 mg | 在庫あり | ¥ 18,500 | |||
25 mg | 在庫あり | ¥ 37,500 | |||
50 mg | 在庫あり | ¥ 56,000 | |||
100 mg | 在庫あり | ¥ 82,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,500 |
説明 | lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM). |
ターゲット&IC50 | SERT:61 nM (Ki), 5-HT2A receptor:0.54 nM (Ki) |
In vitro | Lumateperone also possesses an affinity for the D1 receptor (Ki: 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki: 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold). |
別名 | ITI-007 |
分子量 | 565.7 |
分子式 | C31H36FN3O4S |
CAS No. | 1187020-80-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 245 mg/mL (433.09 mM)
You can also refer to dose conversion for different animals. 詳細
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lumateperone Tosylate 1187020-80-9 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor ITI-007 schizophrenia Inhibitor inhibit dopamine D1 receptor 5-HT2A 5-hydroxytryptamine Receptor ITI 007 presynaptic D2 receptor Lumateperone ITI007 postsynaptic D2 receptor Serotonin Receptor inhibitor