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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $47 | In Stock | |
10 mg | $80 | In Stock | |
25 mg | $163 | In Stock | |
50 mg | $243 | In Stock | |
100 mg | $359 | In Stock | |
1 mL x 10 mM (in DMSO) | $59 | In Stock |
Description | 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). |
Targets&IC50 | 5-HT2A receptor:0.54 nM (Ki), SERT:61 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). |
Alias | ITI-007 |
Molecular Weight | 565.7 |
Formula | C31H36FN3O4S |
Cas No. | 1187020-80-9 |
Smiles | Cc1ccc(cc1)S(O)(=O)=O.CN1CCN2C3CCN(CCCC(=O)c4ccc(F)cc4)CC3c3cccc1c23 |
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: 245 mg/mL (433.09 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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