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

AS2030680 是一种可穿透血脑屏障、口服活性的 5-HT5A 受体拮抗剂。AS2030680 可调控 5-HT5A 相关的下游信号通路,降低乳腺癌细胞中肿瘤球起始细胞的频率,并在动物模型中发挥促认知活性。AS2030680 可用于研究与痴呆、精神分裂症相关的认知障碍以及乳腺癌。

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AS2030680

AS2030680 Chemical Structure

CAS No. : 2170562-35-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

AS2030680 (0.03-30 nM; 60 min) 可强效结合重组人源、大鼠源及小鼠源 5-HT5A 受体,对应的 Ki 值分别为 0.58 nM、1.1 nM 和 2.6 nM[1]
AS2030680 (72 h) 可抑制人乳腺癌细胞 HCC1954 的肿瘤球形成并降低其细胞活力,对应的 IC50 值分别为 1.8 μM 和 3.9 μM[2]
AS2030680 (72 h) 可抑制 MCF-7 人乳腺癌细胞的肿瘤球形成并降低细胞活力,对应的 IC50 值分别为 2.0 μM 和 5.6 μM[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

药代动力学
(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
体内研究
(In Vivo)

AS2030680 (0.001-0.03 mg/kg;口服;一次) 可显著改善 Scopolamine (HY-N0296) 诱导的小鼠工作记忆障碍,且不改变其自发活动[1]
AS2030680 (0.01-0.3 mg/kg;口服;每日;连续 4 天) 显著改善老年大鼠的年龄相关性参考记忆障碍[1]

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.
分子量

428.20

Formula

C17H13BrF3N3O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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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.

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产品名称:
AS2030680
目录号:
HY-182695
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