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 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.

For research use only. We do not sell to patients.

MK-3901

MK-3901 Chemical Structure

CAS No. : 1149750-69-5

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Description

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)

In Vitro

MK-3901 potently antagonizes the P2X3 receptor in a cell-based patch clamp electrophysiology assay with an IC50 of 24 nM[1].
MK-3901 inhibits UGT1A1 enzyme activity in a cell-free biochemical assay with an IC50 of 1 μM[1].
MK-3901 inhibits CYP2C9 enzyme activity in a human liver microsome-based cell-free biochemical assay with an IC50 of 5.7 μM[1].
MK-3901 (10 μM) activates the pregnane X receptor (PXR) by 47%[1].

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

In Vivo

MK-3901 is demonstrated to induce hyperbilirubinemia in multiple species in preclinical studies[1].

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

Molecular Weight

481.53

Formula

C28H24FN5O2

CAS No.
SMILES

C(N[C@H](C)C1=CC=C(F)C=N1)(=O)C2=CC(=CC(=C2)C3=CC=C(C)C=N3)C=4C[C@H](ON4)C5=CC=CC=N5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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MK-3901
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HY-122163
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