BGC-201259

BGC-201259 (RS-1259) is an orally active inhibitor that simultaneously targets acetylcholinesterase (AChE) (IC50 = 101 nM) and serotonin transporter (SERT) (IC50 = 42 nM) . BGC-201259 inhibits 5-HT receptor with an IC50 of 90 nM. BGC-201259 exhibits strong weak activity against the NA transporter (IC50 = 7.7 μM), L-type calcium channel (IC50 = 3.6 μM), σ receptor (IC50 = 2 μM), and sodium channel (IC50 = 5.1 μM) . BGC-201259 demonstrates synergistic potential in improving cognitive and emotional symptoms by balancing the inhibition of these two targets. BGC-201259 can be used in research on Alzheimer's disease[1][2].

Product Specifications

CAS Number

[444667-97-4]

Product Name Alternative

RS-1259

UNSPSC

12352005

Target

5-HT Receptor; Calcium Channel; Cholinesterase (ChE) ; Serotonin Transporter; Sigma Receptor; Sodium Channel

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Smiles

CN[C@H](C1=CC=C(OC(N(C)C)=O)C=C1)CCOC2=CC=C([N+]([O-])=O)C=C2.CN[C@H](C3=CC=C(OC(N(C)C)=O)C=C3)CCOC4=CC=C([N+]([O-])=O)C=C4.O=C(O)/C=C/C(O)=O

Molecular Formula

C42H50N6O14

Molecular Weight

862.88

References & Citations

[1]Abe Y, et al. Pharmacological characterization of RS-1259, an orally active dual inhibitor of acetylcholinesterase and serotonin transporter, in rodents: possible treatment of Alzheimer's disease. J Pharmacol Sci. 2003 Sep;93 (1) :95-105. |[2]Toda N, Kaneko T, Kogen H. Development of an efficient therapeutic agent for Alzheimer's disease: design and synthesis of dual inhibitors of acetylcholinesterase and serotonin transporter. Chem Pharm Bull (Tokyo) . 2010 Mar;58 (3) :273-87.