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lumateperone Tosylate

Catalog No. TQ0084   CAS 1187020-80-9
Synonyms: ITI-007

lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).

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lumateperone Tosylate Chemical Structure
lumateperone Tosylate, CAS 1187020-80-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 47.00
10 mg In stock $ 80.00
25 mg In stock $ 163.00
50 mg In stock $ 243.00
100 mg In stock $ 359.00
1 mL * 10 mM (in DMSO) In stock $ 59.00
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Purity: 98.57%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description lumateperone Tosylate (ITI-007) is a 5-HT2A receptor antagonist (Ki: 0.54 nM), a SERT blocker (Ki: 61 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki: 32 nM).
Targets&IC50 SERT:61 nM (Ki), 5-HT2A receptor:0.54 nM (Ki)
In vitro Lumateperone also possesses an 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).
Synonyms ITI-007
Molecular Weight 565.7
Formula C31H36FN3O4S
CAS No. 1187020-80-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 245 mg/mL (433.09 mM)

TargetMolReferences and Literature

1. Vyas P, et al. An evaluation of lumateperone tosylate for the treatment of schizophrenia. Expert Opin Pharmacother. 2020 Feb;21(2):139-145.

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library GPCR Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Clinical Compound Library Neurotransmitter Receptor Compound Library Covalent Inhibitor Library

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Keywords

lumateperone Tosylate 1187020-80-9 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor ITI-007 schizophrenia Inhibitor inhibit dopamine D1 receptor 5-HT2A 5-hydroxytryptamine Receptor ITI 007 presynaptic D2 receptor Lumateperone ITI007 postsynaptic D2 receptor Serotonin Receptor inhibitor

 

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