1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
    Dopamine Receptor
  3. Lumateperone tosylate

Lumateperone tosylate (Synonyms: ITI-007 tosylate)

Cat. No.: HY-19733 Purity: 99.42%
Handling Instructions

Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

For research use only. We do not sell to patients.

Lumateperone tosylate Chemical Structure

Lumateperone tosylate Chemical Structure

CAS No. : 1187020-80-9

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10 mM * 1 mL in DMSO USD 149 In-stock
Estimated Time of Arrival: December 31
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ready for reconstitution
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10 mg USD 180 In-stock
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50 mg USD 540 In-stock
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100 mg USD 900 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia[1][2][3].

IC50 & Target

5-HT2A Receptor

0.54 nM (Ki)

In Vitro

Lumateperone (2-30 μM) tosylate has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: RPMI-8226 cells
Concentration: 2-30 μM
Incubation Time:
Result: Inhibited cell growth with the IC50 value of 17.30 μM.
In Vivo

Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male Sprague-Dawley rats[2]
Dosage: 1-10 mg/kg
Administration: Intraperitoneal injection
Result: Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes.
Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.
Clinical Trial
Molecular Weight

565.70

Formula

C31H36FN3O4S

CAS No.
SMILES

O=C(C1=CC=C(F)C=C1)CCCN2CC[[email protected]@](N3CCN(C)C4=C3C5=CC=C4)([H])[[email protected]@]5([H])C2.O=S(C6=CC=C(C)C=C6)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (176.77 mM; Need ultrasonic)

H2O : 1 mg/mL (1.77 mM; ultrasonic and warming and heat to 80°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7677 mL 8.8386 mL 17.6772 mL
5 mM 0.3535 mL 1.7677 mL 3.5354 mL
10 mM 0.1768 mL 0.8839 mL 1.7677 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.42%

References
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Product Name:
Lumateperone tosylate
Cat. No.:
HY-19733
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