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

Lumateperone  (Synonyms: ITI-007)

Cat. No.: HY-17637 Purity: 99.83%
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Lumateperone (ITI-007) is an orally active 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 has anticancer activity and can also be used for the study of schizophrenia and bipolar depression.

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

Lumateperone Chemical Structure

Lumateperone Chemical Structure

CAS No. : 313368-91-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Lumateperone:

Lumateperone Related Antibodies

Top Publications Citing Use of Products

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Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

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Description

Lumateperone (ITI-007) is an orally active 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 has anticancer activity and can also be used for the study of schizophrenia and bipolar depression[1][2][3].

IC50 & Target

D1 Receptor

 

D2 Receptor

 

In Vitro

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

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

Lumateperone Related Antibodies

Cell Proliferation Assay[1]

Cell Line: RPMI-8226 cells
Concentration: 2-30 μM
Incubation Time: 48 hours
Result: Inhibited cell growth with the IC50 value of 17.30 μM.
In Vivo

Lumateperone (i.p., 1-10 mg/kg) promotes NMDA and AMPA-induced currents in a dopamine D1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices[2].

MedChemExpress (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

393.50

Formula

C24H28FN3O
CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

CN1C2=C3C([C@@]4([H])[C@@](CCN(C4)CCCC(C5=CC=C(C=C5)F)=O)([H])N3CC1)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (317.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5413 mL 12.7065 mL 25.4130 mL
5 mM 0.5083 mL 2.5413 mL 5.0826 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5413 mL 12.7065 mL 25.4130 mL 63.5324 mL
5 mM 0.5083 mL 2.5413 mL 5.0826 mL 12.7065 mL
10 mM 0.2541 mL 1.2706 mL 2.5413 mL 6.3532 mL
15 mM 0.1694 mL 0.8471 mL 1.6942 mL 4.2355 mL
20 mM 0.1271 mL 0.6353 mL 1.2706 mL 3.1766 mL
25 mM 0.1017 mL 0.5083 mL 1.0165 mL 2.5413 mL
30 mM 0.0847 mL 0.4235 mL 0.8471 mL 2.1177 mL
40 mM 0.0635 mL 0.3177 mL 0.6353 mL 1.5883 mL
50 mM 0.0508 mL 0.2541 mL 0.5083 mL 1.2706 mL
60 mM 0.0424 mL 0.2118 mL 0.4235 mL 1.0589 mL
80 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7942 mL
100 mM 0.0254 mL 0.1271 mL 0.2541 mL 0.6353 mL
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Lumateperone Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lumateperone313368-91-1ITI-007ITI007ITI 007Dopamine Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2Apresynaptic D2 receptorpostsynaptic D2 receptordopamine D1 receptorschizophreniaInhibitorinhibitorinhibit

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