1. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  2. P2X Receptor UGT Cytochrome P450 Pregnane X Receptor (PXR)
  3. MK-3901

MK-3901 是一种选择性的 P2X3 受体拮抗剂,其 IC50 为 24 nM。MK-3901 抑制 UGT1A1 (IC50 为 1 μM) 与 CYP2C9 (IC50 为 5.7 μM)。MK-3901 可激活 PXR。MK-3901 诱发高胆红素血症。MK-3901 可用于炎性疼痛的研究。

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MK-3901

MK-3901 Chemical Structure

CAS No. : 1149750-69-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain[1].

IC50 & Target[1]

P2X3 Receptor

24 nM (IC50)

CYP2C9

5.7 μM (IC50)

UGT1A1

1 μM (IC50)

体外研究
(In Vitro)

MK-3901 在基于细胞的膜片钳电生理实验中可强效拮抗 P2X3 受体,其 IC50 为 24 nM[1]
MK-3901 在无细胞生化分析中抑制 UGT1A1 酶活性,其 IC50 为 1 μM[1]
MK-3901 在基于肝微粒体的无细胞生化分析中可抑制 CYP2C9 酶活性,其 IC50 为 5.7 μM[1]
MK-3901 (10 μM) 可激活孕烷 X 受体 (PXR),激活率达 47%[1]

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

体内研究
(In Vivo)

MK-3901 在临床前研究中被证明可导致多种物种出现高胆红素血症[1]

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

分子量

481.53

Formula

C28H24FN5O2

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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  • 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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HY-122163
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