2. GPCR/G Protein
  3. Bradykinin Receptor
  4. MK 0686

MK 0686是一种强效的缓激肽 (Bradykinin) B1 受体拮抗剂，具有自动诱导代谢的特性。口服给药后，MK 0686 在卷尾猴体内经过氧化途径发生显著生物转化，形成代谢物 M11 和 M13。这种代谢诱导主要由 CYP2C75 介导，表现为该酶 mRNA 表达、蛋白质水平和催化活性的增加。自动诱导现象说明 MK 0686 能通过上调 CYP2C75 增强自身代谢，可能影响其长期药代动力学。

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MK 0686 Chemical Structure

MK 0686 Chemical Structure

CAS No. : 578727-68-1

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MK 0686 相关抗体

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Bradykinin B1 Receptor (B1R) Bradykinin B2 Receptor (B2R)

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
1.52 nM
Compound: 13b
Activity at human bradykinin B1 receptor assessed as inhibition of Des-arg kallidin-induced increase of cytosolic calcium in CHO cells by FLIPR
Activity at human bradykinin B1 receptor assessed as inhibition of Des-arg kallidin-induced increase of cytosolic calcium in CHO cells by FLIPR
[PMID: 17228869]
分子量

486.84

Formula

C22H19ClF4N2O4
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

MK 0686 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

MK 0686578727-68-1MK0686MK-0686Bradykinin ReceptorInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-15042
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