2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. 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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AS2030680

AS2030680 Chemical Structure

CAS No. : 2170562-35-1

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AS2030680 Related Antibodies

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Description

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[1][2][3].

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route Plasma Concentration Brain Concentration
Rat[1] 0.1 mg/kg p.o. 3.0 ng/mL 1.6
Rat[1] 0.1 mg/kg p.o. 0.4 ng/mL 0.1
In Vivo

AS2030680 (0.001-0.03 mg/kg; p.o.; single administration) significantly ameliorates Scopolamine (HY-N0296)-induced working memory impairment in mice without altering their spontaneous activity[1].
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.

Animal Model: ddY mice (male, 5-6 weeks old, Scopolamine-induced working memory deficit)[1]
Dosage: 0.001 mg/kg; 0.003 mg/kg; 0.01 mg/kg; 0.03 mg/kg
Administration: p.o.; single administration
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.
Animal Model: Fischer 344 rats (male, 25 months old, age-related reference memory deficit)[1]
Dosage: 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
Administration: p.o.; daily; 4 days
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.
Molecular Weight

428.20

Formula

C17H13BrF3N3O2
CAS No.
SMILES

O=C(C1=CC2=C(OCC=C2C3=C(F)C=C(F)C=C3F)C=C1)NC(N)=N.Br
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AS2030680 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AS20306802170562-35-1AS 2030680AS-20306805-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorschizophreniabreast cancerMCF-7 human breast tumor cells5-HT5A receptormiceHCC1954 human breast tumor cellsratscognitive impairmentdementiabreast cancer cellsInhibitorinhibitorinhibit

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