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Brilaroxazine

Catalog No. T14782 CAS 1239729-06-6

Synonyms: RP5063

Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.

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Brilaroxazine, CAS 1239729-06-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 132.00
5 mg	In stock	$ 328.00
10 mg	In stock	$ 563.00
25 mg	In stock	$ 891.00
50 mg	In stock	$ 1,230.00
100 mg	In stock	$ 1,670.00
500 mg	In stock	$ 3,350.00
1 mL * 10 mM (in DMSO)	In stock	$ 387.00

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Purity: 98%

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Description	Brilaroxazine (RP5063) is a potent multimodal dopamine/5-HT modulator. Brilaroxazine is a partial agonist of dopamine D2, D3, and D4 receptors, 5-HT1A (Ki =1.5 nM) and 5-HT2A (Ki = 2.5 nM), and has antagonist activity 5-HT2B, and 5-HT7 receptors with Kis of 0.19 nM and 2.7 nM, respectively. Brilaroxazine can be used for research about cognitive impairments in neuropsychiatric and neurological diseases.
Targets&IC50	5-HT1A receptor:1.5 nM (Ki), 5-HT7 receptor:2.7 nM (Ki), 5-HT2A receptor:2.5 nM (Ki), 5-HT2B receptor:0.19 nM (Ki)
In vivo	Brilaroxazine (10 mg/kg) had efficacy in PAH, and mitigated the functional and structural effects of MCT-induced PAH, with significant improvements in pulmonary hemodynamics, right ventricular (RV) hypertrophy, SO2, and pulmonary blood vessel structural changes[3].

Synonyms	RP5063
Molecular Weight	450.36
Formula	C22H25Cl2N3O3
CAS No.	1239729-06-6

Storage

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

Solubility Information

DMSO: 95 mg/mL (210.94 mM), Sonication is recommended.

References and Literature

1. Bhat L, et al. Evaluation of the effects of RP5063, a novel, multimodal, serotonin receptor modulator, as single-agent therapy and co-administrated with sildenafil, bosentan, and treprostinil in a monocrotaline-induced pulmonary arterial hypertension rat 2. Bhat L, et al. Evaluation of the effects of RP5063, a novel, multimodal, serotonin receptor modulator, as single-agent therapy and co-administrated with sildenafil, bosentan, and treprostinil in a monocrotaline-induced pulmonary arterial hypertension rat model.Eur J Pharmacol. 2018 May 15;827:159-166. 3. L. Bhat,et al. Rp5063 Prevents Monocrotaline Induced Pulmonary Arterial Hypertension In Rats. 4. Reviva Pharmaceuticals Reports RP5063 Positive Efficacy Results for Memory Deficits

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library GPCR Compound Library Anti-Cancer Clinical Compound Library Neuronal Signaling Compound Library Antidepressant Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Brilaroxazine 1239729-06-6 GPCR/G Protein Neuroscience Dopamine Receptor 5-HT Receptor Parkinson depressive hypertension cardiac syndrome,ADHD autism inhibit Pulmonary RP5063 PAH Serotonin Receptor Alzheimer RP 5063 Inhibitor RP-5063 disorder,Tourette arterial 5-hydroxytryptamine Receptor inhibitor

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