lumateperone Tosylate

SKU: orb1296216

Description

Lumateperone tosylate (ITI-007) is a multifunctional small molecule acting as a potent 5-HT2A receptor antagonist, a serotonin transporter (SERT) blocker, and a dopamine D2 receptor modulator with presynaptic partial agonism and postsynaptic antagonism. It is utilized in preclinical research for investigating neuropsychiatric disorders, including schizophrenia and mood disorders, in both in vitro and in vivo models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1187020-80-9
• MW: 565.7
• Purity: 99.95% (May vary between batches)
• Formula: C₃₁H₃₆FN₃O₄S
• SMILES: Cc1ccc(cc1)S(O)(=O)=O.CN1CCN2C3CCN(CCCC(=O)c4ccc(F)cc4)CC3c3cccc1c23
• Target: Dopamine Receptor,5-HT Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (8.84 mM);DMSO:250 mg/mL (441.93 mM)

Bioactivity

• Target 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).

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dopamine Receptor, Dopamine, dopamine D1 receptor, DopamineReceptor, 5-HT2A, 5-HT2A antagonist, 5-HT Receptor, 5-hydroxytryptamine Receptor, 5HTReceptor, 5HT Receptor, Lumateperone, lumateperone Tosylate, inhibit, ITI007, ITI-007, ITI 007, Inhibitor, postsynaptic D2 receptor, Serotonin Receptor, presynaptic D2 receptor, SERT, schizophrenia

Compound Identifiers

PubChem CID

74962731