RIMEGEPANT

RIMEGEPANT : Antagonist of CRCP

Structure

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Probe RIMEGEPANT is in the process of SERP review.

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Information

CRCP

Antagonist

up to 100 nM

In Vitro Validations

Uniprot ID: O75575

Target Class: CGRP-receptor component protein

Target SubClass: --

Potency: Ki

Potency Value: 0.027 ± 0.009 nM

Potency Assay: Inhibition of 125I-CGRP binding to SK-N-MC cell membranes

PDB ID for probe-target interaction (3D structure): --

Target aliases:

DNA-directed RNA polymerase III subunit RPC9, CRCP ...

DOI Reference: 10.1021/jm3013147

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Off Target: AMY1A

Potency end-point : IC50 170 nM

Potency assay (off target): BMS-927711 exhibited no significant off-target liabilities when tested against a range of 45 receptors, ion channels and enzymes, and in a panel of hCYP isoforms inhibition of only CYP3A4 was detected (IC50 = 17 μM). It caused <30% inhibition of hERG and had no significant effects on L-type sodium or calcium channels (all tested in HEK-293 cells).

Probe Selectivity in Vitro:

Rimegepant completely blocked activation of the CGRP and AMY1 receptors but was approximately 17-fold more effective at blocking the CGRP receptor (DOI: 10.3389/fphar.2020.01240).

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(last updated: 13 Feb 2025 )