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Brexpiprazole

Catalog No. T2306   CAS 913611-97-9
Synonyms: OPC-34712

Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.

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Brexpiprazole Chemical Structure
Brexpiprazole, CAS 913611-97-9
Pack Size Availability Price/USD Quantity
5 mg In stock $ 45.00
10 mg In stock $ 61.00
25 mg In stock $ 73.00
50 mg In stock $ 85.00
100 mg In stock $ 101.00
200 mg In stock $ 150.00
500 mg In stock $ 288.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.96%
Purity: 99.69%
Purity: 99.54%
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Biological Description
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Description Brexpiprazole (OPC-34712) is a partial agonist of human 5-hydroxytryptamine (5-HT) 5-HT1A and dopamine D2 receptors.
Targets&IC50 Dopamine D2L:0.3 nM(Ki), 5-HT1A:0.12 nM(Ki), hμMan noradrenergic α1B:0.17 nM(Ki), 5-HT2A receptors:0.47 nM(Ki), α2C receptors:0.59 nM(Ki)
In vitro Brexpiprazole is a potent partial agonist at human 5-hydroxytryptamine (5-HT) 5-HT1A (Ki=0.12 nM) and dopamine D2L (Ki=0.3 nM) receptors, and an antagonist at 5-HT2A receptors (Ki=0.47 nM). It also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2Creceptors (Ki=0.59 nM). Furthermore, this drug displays moderate affinity for human D3, 5-HT2B and 5-HT7 receptors, as well as α1A, and α1D adrenergic receptors. Brexpiprazole potentiated NGF-induced neurite outgrowth in PC12 cells. It could significantly potentiate the effects of fluoxetine (or paroxetine) on neurite outgrowth[1].
In vivo Brexpiprazole is able to ameliorate PCP- 191 induced cognitive deficits in mice, via 5-HT1A receptors[2].
Cell Research 2.5 ng/ml of NGF(nerve growth factor) is used to study the potentiating effects of brexpiprazole on neurite outgrowth. Twenty-four hours after plating, the medium is replaced with DMEM medium containing 0.5% FBS and 1% penicillin-streptomycin with NGF (2.5 ng/ml), with or without brexpiprazole (0.001, 0.01, 0.1 or 1.0 μM). Four days after incubation with NGF (2.5 ng/ml) with or without drugs, morphometric analysis is performed on digitized images of live cells taken under phase-contrast illumination, with an inverted microscope linked to a camera. (Only for Reference)
Synonyms OPC-34712
Molecular Weight 433.57
Formula C25H27N3O2S
CAS No. 913611-97-9

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 23 mg/mL (53 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Ishima T, et al. Eur Neuropsychopharmacol. 2015, 25(4):505-511. 2. Yoshimi N, et al. Pharmacol Biochem Behav. 2014, 124:245-249.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Alzheimer's Disease Compound Library Drug-induced Liver Injury (DILI) Compound Library Pediatric Drug Library Anti-Cancer Compound Library NO PAINS Compound Library Neuronal Signaling Compound Library

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Keywords

Brexpiprazole 913611-97-9 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Adrenergic Receptor Serotonin Receptor Beta Receptor PC12 OPC-34712 5-hydroxytryptamine Receptor Inhibitor recognition deficits OPC34712 OPC 34712 antipsychotic orally active inhibit neurite outgrowth inhibitor

 

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