2. GPCR/G Protein Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  3. CCR Histamine Receptor Calcium Channel
  4. YM-344484

YM-344484 是一种具有口服活性的趋化因子 CCR3 受体 (CCR3 receptor) 与组胺 H1 受体 (histamine H1 receptor) 双重拮抗剂。YM-344484 可抑制配体诱导的 Ca2+ 内流，表达 CCR3 的细胞趋化作用， Histamine 诱导的 Ca2+ 内流、血管通透性升高以及嗜酸性粒细胞聚集。YM-344484 抑制血管通透性，在小鼠哮喘模型中，抑制嗜酸性粒细胞浸润。YM-344484 可用于哮喘、过敏性鼻炎及特应性皮炎的相关研究。

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YM-344484

YM-344484 Chemical Structure

CAS No. : 671205-14-4

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YM-344484 相关抗体

Top Publications Citing Use of Products

查看 CCR 亚型特异性产品:

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

查看 Histamine Receptor 亚型特异性产品:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

查看 Calcium Channel 亚型特异性产品:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis[1].

IC50 & Target[1]

CCR3

 

H1 Receptor

 

体外研究
(In Vitro)

YM-344484 可强效抑制表达人 CCR3 的 B300-19 细胞中由 CCR3 配体诱导的钙内流，其 Kβ 值根据配体不同在 0.69 nM 至 2.5 nM 之间波动[1]。
YM-344484 可抑制小鼠 CCR3 表达细胞中由小鼠 CCL11 诱导的钙内流，其 Kβ 值为 88 nM[1]。
YM-344484 可抑制 PC3 细胞中组胺 H1 受体介导的钙内流，其 Kβ 值为 47 nM[1]。
YM-344484 (10 μM) 对 C6 细胞中血清素 5-HT2A 受体介导的钙内流仅表现出微弱的抑制活性，抑制率仅为 25%[1]。
YM-344484 可强效抑制人源 CCR3 表达 B300-19 细胞中 CCR3 配体诱导的趋化作用，其 IC50 值随配体不同在 2.0 nM 至 8.0 nM 之间变化[1]。
YM-344484 可抑制 CCL11 诱导的人外周血嗜酸性粒细胞释放嗜酸性粒细胞源性神经毒素，其 IC50 为 19 nM[1]。

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

YM-344484 相关抗体:
体内研究
(In Vivo)

YM-344484 (3-30 mg/kg；口服；单次给药) 在 10 mg/kg 单次给药剂量下对小鼠小鼠 Histamine (HY-B1204) 诱导的血管通透性抑制率达 82%，30 mg/kg 剂量下可实现完全抑制[1]。
YM-344484 (100-600 mg/kg；口服；每 8 小时 1 次；共 6 剂) 在小鼠 Ovalbumins (HY-W250978) 诱导的哮喘模型中，300 mg/kg 剂量下可抑制 74%的嗜酸性粒细胞浸润，600 mg/kg 剂量下则可完全抑制嗜酸性粒细胞浸润[1]。

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

Animal Model: Balb/c (female, 6 weeks old)[1]
Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Suppressed histamine-induced vascular permeability dose-dependently.
Achieved statistically significant 82% inhibition at 10 mg/kg.
Achieved complete inhibition at 30 mg/kg.
Animal Model: Balb/c (female)[1]
Dosage: 100 mg/kg; 300 mg/kg; 600 mg/kg
Administration: p.o.; every 8 hours; 6 doses
Result: Failed to reduce eosinophil numbers at 100 mg/kg.
Significantly attenuated eosinophil infiltration with 74% inhibition at 300 mg/kg.
Achieved 100% inhibition of eosinophil infiltration at 600 mg/kg.
Exhibited no inhibitory effect on neutrophil or mononuclear cell counts in bronchoalveolar lavage fluid.
分子量

487.57

Formula

C28H30FN5O2
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

YM-344484 相关分类

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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:

YM-344484671205-14-4YM344484YM 344484CCRHistamine ReceptorCalcium ChannelCC chemokine receptorCa2+ channelsCa channelshuman peripheral blood eosinophilshistamine H1 receptorallergic rhinitisC6 cellsatopic dermatitisCCR3 receptorG-protein-coupled receptorsasthmaB300-19 cellsPC3 cellsInhibitorinhibitorinhibit

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