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Cat. No.: HY-122163

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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.

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CAS No.: 1149750-69-5
Formule: C₂₈H₂₄FN₅O₂
Masse moléculaire:481.53

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

MK-3901 Chemical Structure

CAS No.: 1149750-69-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

IC₅₀ & Target^[1]

P2X3 Receptor

24 nM (IC₅₀)

CYP2C9

5.7 μM (IC₅₀)

UGT1A1

1 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform P2X Receptor :

Voir tous les produits spécifiques à Isoform Cytochrome P450 :

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.

Chemical Information

CAS No. 1149750-69-5
Masse moléculaire 481.53
Formule C₂₈H₂₄FN₅O₂
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Ginnetti AT, et al. Identification of second-generation P2X3 antagonists for treatment of pain. Bioorg Med Chem Lett. 2018;28(8):1392-1396. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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MK-3901

Voir tous les produits spécifiques à Isoform P2X Receptor

Voir tous les produits spécifiques à Isoform Cytochrome P450

Activité biologique

Chemical Information

Pureté et documentation

Références

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MK-3901 Related Classifications

HY-122163 Related Classifications