Masupirdine mesylate  (Synonyms: SUVN-502 mesylate)

Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally active, and brain-penetrating 5-HT₆ receptor antagonist (K_i of 2.04 nM for human 5-HT₆ receptor). Masupirdine mesylate 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 mesylate can be used in the research of Alzheimer's disease^[1][2].

Masupirdine (10 μM) mesylate 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.

Masupirdine (1-10 mg/kg; p.o) mesylate exerts procognitive effects on acquisition, consolidation, and retention phases of memory in adult male Wistar rats, and reverses memory deficits induced by Scopolamine (HY-N0296), Scopolamine/MK-801 (HY-15084B), or senescence^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

670.61

C₂₃H₃₂BrN₃O₉S₃

1791396-46-7

Solid

Pale purple to purple

CS(=O)(O)=O.O=S(N1C2=CC=C(OC)C=C2C(CN3CCN(C)CC3)=C1)(C(C=CC=C4)=C4Br)=O.CS(=O)(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]