444667-97-4
Chemical Structure
BGC-201259
Synonym(s): RS-1259
- CAS. Nr.: 444667-97-4
- Formula:C42H50N6O14
- Molecular Weight:862.88
IUPAC Name: (S)-4-(1-(methylamino)-3-(4-nitrophenoxy)propyl)phenyl dimethylcarbamate hemifumarate
InChIKey: JOSUCKKYZJUIPW-SOBORHNCSA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
