Lumateperone
Based on 1 Customer Validation
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.
- Purity: 99.83%
- CAS No.: 313368-91-1
- Formula: C24H28FN3O
- Molecular Weight:393.50
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
|
D1 Receptor |
D2 Receptor |
5-HT2A Receptor |
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.
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Cell Line:RPMI-8226 cells
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Concentration:2-30 μM
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Incubation Time:48 hours
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Result:Inhibited cell growth with the IC50 value of 17.30 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats[2]
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Dosage:1-10 mg/kg
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Administration:Intraperitoneal injection
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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.
Chemical Information
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CAS No. 313368-91-1
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Appearance Oil
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Molecular Weight 393.50
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Formula C24H28FN3O
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Color Light yellow to yellow
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SMILES
CN1C2=C3C([C@@]4([H])[C@@](CCN(C4)CCCC(C5=CC=C(C=C5)F)=O)([H])N3CC1)=CC=C2
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Synonyms
ITI-007
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (254.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Jinyuan Zhang, et al. Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent c-Myc G-quadruplex Stabilizers to Suppress c-Myc Transcription and Myeloma Growth. Mol Inform. 2022 Mar 30:e2200011. [Content Brief]
[2]. J Titulaer, et al. Lumateperone-mediated effects on prefrontal glutamatergic receptor-mediated neurotransmission: A dopamine D1 receptor dependent mechanism. Eur Neuropsychopharmacol. 2022 Jul 22;62:22-35. [Content Brief]
[3]. Lumateperone
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 |