AS2030680
AS2030680 is a blood-brain barrier-permeable, orally active 5-HT5A receptor antagonist. AS2030680 regulates 5-HT5A-related downstream signaling pathways, reduces the frequency of tumorsphere-initiating cells in breast cancer cells, and exerts procognitive activity in animal models. AS2030680 can be used to study cognitive impairments associated with dementia and schizophrenia, as well as breast cancer.
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- No. CAS: 2170562-35-1
- Fòrmula: C17H13BrF3N3O2
- Peso molecular:428.20
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
AS2030680 (0.03-30 nM; 60 min) potently binds to recombinant human, rat, and mouse 5-HT5A receptors, with corresponding Ki values of 0.58 nM, 1.1 nM, and 2.6 nM, respectively[1].
AS2030680 (72 h) inhibits tumor sphere formation and reduces cell viability in human breast cancer cell line HCC1954, with corresponding IC50 values of 1.8 μM and 3.9 μM[2].
AS2030680 (72 h) inhibits tumor sphere formation and reduces cell viability in MCF-7 human breast cancer cells, with corresponding IC50 values of 2.0 μM and 5.6 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AS2030680 (0.01-0.3 mg/kg; p.o.; daily; for 4 consecutive days) significantly ameliorates age-related reference memory impairment in aged rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 5-6 weeks old, Scopolamine-induced working memory deficit)[1]
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Dosage:0.001 mg/kg; 0.003 mg/kg; 0.01 mg/kg; 0.03 mg/kg
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Administration:p.o.; single administration
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Result:Did not produce a statistically significant improvement in the scopolamine-induced decrease in Y-maze alternation rate at the 0.001 mg/kg dose.
Significantly restored the scopolamine-induced decrease in Y-maze alternation rate at the 0.003 mg/kg, 0.01 mg/kg, and 0.03 mg/kg doses.
Did not affect the number of arm entries (a measure of locomotor activity) at any tested dose.
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Animal Model:Fischer 344 rats (male, 25 months old, age-related reference memory deficit)[1]
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Dosage:0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; daily; 4 days
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Result:Significantly reduced the 4-day cumulative escape latency in aged rats at the 0.03 mg/kg and 0.1 mg/kg doses, indicating improved reference memory.
Did not produce statistically significant reductions in cumulative latency at the 0.01 mg/kg and 0.3 mg/kg doses.
Reduced daily escape latencies across the training period at the 0.03 mg/kg and 0.1 mg/kg doses compared to vehicle-treated aged rats.
Chemical Information
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No. CAS 2170562-35-1
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Peso molecular 428.20
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Fòrmula C17H13BrF3N3O2
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SMILES
O=C(C1=CC2=C(OCC=C2C3=C(F)C=C(F)C=C3F)C=C1)NC(N)=N.Br
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Yamazaki M, et al. Novel 5-HT5A receptor antagonists ameliorate scopolamine-induced working memory deficit in mice and reference memory impairment in aged rats. J Pharmacol Sci. 2015 Mar;127(3):362-9. [Content Brief]
[2]. Gwynne WD, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020;20(1):724. Published 2020 Aug 5. [Content Brief]
[3]. Garay RP, et al. Potential serotonergic agents for the treatment of schizophrenia. Expert Opin Investig Drugs. 2016;25(2):159-170. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AS2030680 Related Classifications
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