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.
- CAS No.: 1149750-69-5
- Formula: C28H24FN5O2
- Molecular Weight:481.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All P2X Receptor Isoforms
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Biological Activity
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P2X3 Receptor 24 nM (IC50) |
CYP2C9 5.7 μM (IC50) |
UGT1A1 1 μM (IC50) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1149750-69-5
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Molecular Weight 481.53
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Formula C28H24FN5O2
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)