2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. PAR4 antagonist 4

PAR4 antagonist 4 (Compound 37) 是蛋白酶激活受体4 (PAR4) 的选择性拮抗剂。PAR4 antagonist 3 具有抗血小板作用，IC50为 14.2 nM。PAR4 antagonist 3 改善人肝微粒体代谢稳定性，T1/2 为 42.5 min。

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PAR4 antagonist 4 Chemical Structure

PAR4 antagonist 4 Chemical Structure

CAS No. : 3057206-41-1

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PAR4 antagonist 4 相关抗体

Top Publications Citing Use of Products

查看 Protease Activated Receptor (PAR) 亚型特异性产品:

查看所有亚型
PAR1 PAR2 PAR4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min[1].

IC50 & Target

PAR4

14.2 nM (IC50)

体外研究
(In Vitro)

PAR4 antagonist 4 (4 μM) 对 GPVI 具有拮抗作用，抑制胶原诱导的血小板聚集信号通路[1]。

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

PAR4 antagonist 4 相关抗体:
体内研究
(In Vivo)

PAR4 antagonist 4 (3-12 mg/kg，口服，单剂量) 抑制 C57BL/J6 小鼠切尾模型出血时间，对凝血系统无影响[1]。
PAR4 antagonist 4 (2 mg/kg，静脉注射或 12 mg/kg，口服) 具有如表格所示的药代动力学特性：

Pharmacokinetic Analysis of PAR4 antagonist 4 in ICR mice[1]

Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0→t (ng·h/mL) Cl (mL/h·kg) F (%)
i.v. 2 mg/kg 38.3 - - 5386 180 -
p.o. 12 mg/kg 29.5 2 204 3042 - 9.61

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

Animal Model: C57BL/J6 mice tail cutting model[1]
Dosage: 3-12 mg/kg
Administration: po, single dose
Result: Suppressed the bleeding time.
分子量

453.44

Formula

C22H16FN3O5S
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

PAR4 antagonist 4 相关分类

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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.

Keywords:

PAR4 antagonist 43057206-41-1Protease Activated Receptor (PAR)Thrombin receptorsC57BL/J6ICRantiplateletatherothrombosisInhibitorinhibitorinhibit

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