cgrp antagonist 1

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a selective calcitonin gene-related peptide 1 (CGRP1) receptor antagonist with an IC50=0.03 nM and Ki=14.4 pM.

Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP).

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

AC 187 TFA, a potent and orally active amylin receptor antagonist, exhibits an IC50 of 0.48 nM and a Ki of 0.275 nM. It demonstrates greater selectivity for the amylin receptor over calcitonin and CGRP receptors and has been shown to possess neuroprotective effects [1] [2].