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: 99.21%
Handling Instructions

Lumateperone tosylate (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 SERT blocker (Ki = 61 nM).

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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Based on 1 publication(s) in Google Scholar

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Description

Lumateperone tosylate (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 SERT blocker (Ki = 61 nM). IC50 value: 0.54 nM (Ki, for 5-HT2A receptor ) Target: 5-HT2A receptor Lumateperone also possesses 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).[1] in vivo: It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone.[1]

IC50 & Target

5-HT2A Receptor

0.54 nM (Ki)

Clinical Trial
Molecular Weight

565.70

Formula

C₃₁H₃₆FN₃O₄S

CAS No.

1187020-80-9

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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

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 provided by MCE.
References

Purity: 99.21%

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Keywords:

LumateperoneITI-007ITI007ITI 0075-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorInhibitorinhibitorinhibit

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