CGRP Receptor Antagonist

Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC₅₀ of 0.03 nM and K_i of 14.4 pM for human CGRP.

Vazegepant (BHV-3500) hydrochloride is a highly affinity CGRP receptor antagonist (hCGRP K_i= 0.023 nM). Vazegepant hydrochloride is the first intranasal gepant for migraine. Vazegepant hydrochloride may be helpful in effective management of COVID-19 associated pulmonary inflammation.

Rimegepant (BMS-927711; BHV-3000) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC₅₀ of 8.01 and a K_i of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .

Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.

Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.

Olcegepant hydrochloride (BIBN-4096 hydrochloride) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC₅₀ of 0.03 nM and with a K_i of 14.4 pM for human CGRP.

MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC₅₀=0.12 nM; K_i=0.024 nM). MK-3207 can be used for migraine studies.

Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.

Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine.

Galcanezumab (LY 2951742) is a humanized IgG4 monoclonal antibody against the CGRP ligand. Galcanezumab can be used for migraine or cluster headaches research.

Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with K_is of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.

Vazegepant (Zavegepant) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. Vazegepant can be used in the study of migraine.

HCGRP-(8-37) (Human α-CGRP (8-37)) is a fragment of human calcitonin gene-related peptide (hCGRP) and an antagonist of the CGRP receptor, with an IC₅₀ of 32.1 pM against the CGRP receptor. HCGRP-(8-37) blocks adenylate cyclase activation induced by CGRP receptor ligands and attenuates vascular responses triggered by CGRP. HCGRP-(8-37) reduces capsaicin-induced vasodilation in porcine nasal mucosa and superficial skin. HCGRP-(8-37) serves as a research tool to distinguish effects mediated by CGRP or calcitonin receptors, and to investigate CGRP-induced vascular effects.

MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

Rimegepant (BMS-927711) sulfate hydrate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor. Rimegepant sulfate hydrate can be used for migraine research.

CGRP antagonist 1 (compound 21) is a highly potent CGRP receptor antagonist with a K_i and an IC₅₀ of 1.7 nM and 5.7 nM, respectively.

CGRP antagonist 2 is a CGRP receptor antagonist. CGRP antagonist 2 can be used for pain relief.

MK-3207 hydrochloride (Standard) is the analytical standard of MK-3207 hydrochloride (HY-10302). This product is intended for research and analytical applications. MK-3207 hydrochloride is a potent and orally bioavailable CGRP receptor antagonist with IC₅₀ of 0.12 nM and K_i of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.

HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute research of migraine.

Rimegepant-d₄ (BMS-927711-d₄) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC₅₀ of 8.01 and a K_i of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine.