| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Rat 5-HT2A ( Ki = 0.54 nM )
Lumateperone targets serotonin 5-HT2A receptors and dopamine D2 receptors. It acts as a dual 5-HT2A receptor antagonist and dopamine receptor phosphoprotein modulator (DPPM). The compound has a unique receptor binding profile that allows it to target schizophrenia-related symptoms while minimizing adverse effects. It lacks presynaptic dopamine D2 antagonism and has low D2 receptor occupancy. |
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| ln Vitro |
Lumateperone HCl(2-30 μM) exhibits anti-tumor activity and has the ability to dose-dependently inhibit cell proliferation[1].
In vitro, lumateperone HCl (2-30 μM) exhibits anti-tumor activity and has the ability to dose-dependently inhibit cell proliferation. It shows receptor binding affinity for 5-HT2A and dopamine D2 receptors. Detailed in vitro potency data is available in the primary literature. |
| ln Vivo |
Lumateperone (i.p., 1-10 mg/kg) tosylate increases the release of dopamine and glutamate in rat mPFC slices and promotes NMDA and AMPA-induced currents in a manner that is dependent on the dopamine D 1 receptor[2].
In vivo, lumateperone (i.p., 1-10 mg/kg) has been studied in animal models. The compound shows efficacy in schizophrenia models. It is administered orally at a recommended dosage of 42 mg once daily for the treatment of schizophrenia. Dose titration is not required. |
| Enzyme Assay |
Non-cellular receptor binding assays for lumateperone involve radioligand displacement using membrane preparations expressing 5-HT2A or dopamine D2 receptors. Membranes are incubated with radiolabeled ligands and varying concentrations of lumateperone. Bound radioactivity is measured by filtration. Ki values are calculated from competition binding curves.
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| Cell Assay |
Cell Line: RPMI-8226 cells
Concentration: 2-30 μM Result: Inhibited cell growth with the IC50 value of 17.30 μM. In vitro cellular experiments involve cells expressing serotonin or dopamine receptors. Cells are treated with lumateperone, and downstream signaling is measured. Functional activity (agonist/antagonist) is determined by comparing responses to reference agonists. Anti-tumor activity is assessed in cancer cell lines. |
| Animal Protocol |
Adult male Sprague-Dawley rats
1-10 mg/kg Intraperitoneal injection In vivo animal studies involve administration of lumateperone to rodents to assess antipsychotic-like effects. The compound's effects on behavior, including locomotor activity and prepulse inhibition, are evaluated. Specific protocols are described in the primary literature. |
| ADME/Pharmacokinetics |
Lumateperone is orally bioavailable. The recommended dosage for schizophrenia is 42 mg once daily. For moderate or severe hepatic impairment, the recommended dosage is 21 mg once daily. The compound has a favorable safety profile with low risk of extrapyramidal symptoms and metabolic or endocrine adverse effects.
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| Toxicity/Toxicokinetics |
Lumateperone is generally well-tolerated. It has a low risk of extrapyramidal symptoms and metabolic or endocrine adverse effects. The compound is for research purposes only and is not for human therapeutic use in a research setting.
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| References |
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| Additional Infomation |
Lumateperone HCl (ITI-007, ITI-722; Caplyta) is a dual 5-HT2A receptor antagonist and dopamine receptor phosphoprotein modulator (DPPM) approved for the treatment of schizophrenia. It has a unique receptor binding profile that minimizes adverse effects. This product is for research purposes only and is not for human therapeutic use.
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| Molecular Formula |
C24H28FN3O-HCL
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| Exact Mass |
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| Related CAS # |
Lumateperone; 313368-91-1
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| Appearance |
Solid powder
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| InChi Key |
LHAPOGAFBLSJJQ-GUTACTQSSA-N
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| InChi Code |
InChI=1S/C24H28FN3O.C7H8O3S/c1-26-14-15-28-21-11-13-27(16-20(21)19-4-2-5-22(26)24(19)28)12-3-6-23(29)17-7-9-18(25)10-8-171-6-2-4-7(5-3-6)11(8,9)10/h2,4-5,7-10,20-21H,3,6,11-16H2,1H32-5H,1H3,(H,8,9,10)/t20-,21-/m0./s1
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| Chemical Name |
1-(4-fluorophenyl)-4-[(6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4'
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| Synonyms |
ITI-007 HCl; ITI007; Lumateperone; Caplyta; ITI-722; ITI722; ITI 722; ITI 007
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~176.8 mM)
H2O: < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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