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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- CAS. Nr.: 444667-97-4
- Formel: C42H50N6O14
- Molecular Weight:862.88
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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
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
BGC-201259 (64 mg/kg, p.o., single dose) simultaneously enhances cholinergic and serotonergic neurotransmission in the living rat brain[1][2].
BGC-201259 (4-16 mg/kg, p.o., single dose) significantly enhances the locomotor activity induced by 5-HTP and exhibits antidepressant-like activity in mice[1][2].
BGC-201259 (0.5-1 mg/kg, p.o., single dose) significantly improves the spatial short-term memory impairment in aged rats[1][2].
BGC-201259 (1-4 mg/kg, p.o., single dose) dose-dependently increases the period of wakefulness and reduce sleep in rats[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:4, 8, 16 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Significantly enhanced 5-HTP-induced motor activity, exhibiting a bell-shaped dose-response curve.
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Animal Model:
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Dosage:0.5, 1 and 2 mg/kg
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Administration:Oral administration (p.o.), single dose
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Result:Significantly improved spatial short-term memory deficits in aged rats.
Chemical Information
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CAS. Nr. 444667-97-4
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Molecular Weight 862.88
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Formel C42H50N6O14
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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
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Synonyms
RS-1259
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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]. 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]
Calculators
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