Masupirdine free base
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally active, and brain-penetrating 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base has pro-cognitive effects on all stages of cognition (acquisition, consolidation, and retention), and can reverse Scopolamine (HY-N0296), MK-801 (HY-15084B)-induced and aging-related memory deficits. Masupirdine free base can be used in the research of Alzheimer's disease.
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- CAS. Nr.: 701205-60-9
- Formel: C21H24BrN3O3S
- Molecular Weight:478.40
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
5-HT2A Receptor |
5-HT6 Receptor 2.04 nM (Ki) |
In Vitro
Masupirdine (10 μM) free base shows no agonist or partial agonist effects on luciferase activity but blocks serotonin-induced luciferase activity in the 5-HT6 receptor functional assay using CHO-K1 cells stably expressing human 5-HT6 receptor and CRE-Luc reporter gene[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 701205-60-9
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Molecular Weight 478.40
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Formel C21H24BrN3O3S
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SMILES
O=S(N1C2=CC=C(OC)C=C2C(CN3CCN(C)CC3)=C1)(C(C=CC=C4)=C4Br)=O
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Synonyms
SUVN-502 free base
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Nirogi R, et al. Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer's Disease. J Med Chem. 2017 Mar 9;60(5):1843-1859. [Content Brief]
[2]. Nirogi R, et al. SUVN-502, a novel, potent, pure, and orally active 5-HT6 receptor antagonist: pharmacological, behavioral, and neurochemical characterization. Behav Pharmacol. 2019 Feb;30(1):16-35. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Masupirdine free base Related Classifications
HY-109118 Related Classifications
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