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.
For research use only. We do not sell to patients.
- CAS No.: 444667-97-4
- Formula: C42H50N6O14
- Molecular Weight:862.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vivo
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 No. 444667-97-4
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Molecular Weight 862.88
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BGC-201259 Related Classifications
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