2. GPCR/G Protein
  3. P2Y Receptor
  4. P2Y14R antagonist 3

P2Y14R antagonist 3 (compound A) 是一种有口服活性的 P2Y14R 拮抗剂，其IC50 值为 23.60 nM，Kd 值为 7.26 μM。P2Y14R antagonist 3 可减轻 Lipopolysaccharides (LPS) (HY-D1056) 诱发的急性肺损伤小鼠的肺损伤程度。P2Y14R antagonist 3 可用于炎症性疾病研究。

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P2Y14R antagonist 3 Chemical Structure

P2Y14R antagonist 3 Chemical Structure

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P2Y14R antagonist 3 相关抗体

Top Publications Citing Use of Products

查看 P2Y Receptor 亚型特异性产品:

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P2Y14R antagonist 3 (Compound A) is a potent and orally active P2Y14R antagonist with an IC50 value of 23.60 nM and a Kd value of 7.26 μM. P2Y14R antagonist 3 can reduce the degree of lung injury in the Lipopolysaccharides (LPS) (HY-D1056)-induced acute lung injury mice. P2Y14R antagonist 3 can be used for inflammatory diseases[1].

IC50 & Target[1]

P2Y14 Receptor

23.6 nM (IC50)

P2Y14 Receptor

7.26 μM (Kd)

体外研究
(In Vitro)

P2Y14R antagonist 3 对 CYP1A2 和 CYP2C9 没有抑制作用，对 CYP2C19 和 CYP3A4 有较弱的抑制活性，IC50 值分别为 28.6 μM 和 21.3 μM[1]。
P2Y14R antagonist 3 没有表现出心脏毒性副作用，表现出优异的生物药稳定性，在模拟胃液和肠液中表现出抗降解性，在人肝微粒体中保持较高的代谢稳定性，将其归类为低清除率化合物[1]。

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

P2Y14R antagonist 3 相关抗体:
体内研究
(In Vivo)

P2Y14R antagonist 3 (2-6 mg/kg；口服给药；每天一次，连续7天给药) 可减轻 LPS 诱发的急性肺损伤小鼠的肺损伤程度，免疫细胞浸润减少，炎症因子 IL-6、TNF-α、IL-β水平明显降低[1]。

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

Animal Model: LPS-induced acute lung injury male C57BL/6 mice (6-8 weeks)[1]
Dosage: 2 mg/kg, 6 mg/kg
Administration: Oral gavage (p.o.); once daily for 7 days, on the 5th day of the experiment, mice were injected with 25 mg/kg LPS to induce Acute Lung Injury (ALI), and mice were killed 3 h after 7th day administration.
Result: Reduced inflammation and reduced tissue damage, and reduced the content of inflammatory cytokines and the pathological changes of lung tissue in LPS-induced ALI mouse model.
分子量

487.51

Formula

C26H25N5O5
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

P2Y14R antagonist 3 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:

P2Y14R antagonist 3P2Y ReceptorP2Y14R antagonistAnti-inflammatoryInhibitorinhibitorinhibit

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目录号：
HY-172226
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