Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
CGRP receptor antagonists block the receptor for calcitonin gene-related peptide (CGRP), a neuropeptide. In 1982 alternative RNA processing of the calcitonin gene was shown to produce CGRP in neural tissue. The receptor is formed by calcitonin receptor-like receptor (CALCRL) together with receptor activity-modifying protein 1 (RAMP1), as described in 1998. CGRP release from trigeminal neurons is studied in migraine models and in neurogenic vasodilation. Olcegepant, telcagepant, MK-3207 and ubrogepant are small-molecule antagonists of this receptor complex. CGRP 8-37 (human) is a truncated peptide antagonist, and α-CGRP(human) serves as the native agonist.
MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.
Synonyms: MK-0974
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors.
Synonyms: BIBN-4096; BIBN 4096BS
Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect.
MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
Synonyms: HCGRP-(8-37)
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively.
Synonyms: MK-1602
Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
Synonyms: BIBN-4096 hydrochloride; BIBN4096; BIBN4096BS hydrochloride; BIBN 4096BS
Olcegepant hydrochloride is the first potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and with a Ki of 14.4 pM for human CGRP.
Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
Synonyms: 22-52-Adrenomedullin (human
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.
PCC0105005 is a potent CGRP receptor antagonist, exhibiting an IC50 of 1.01 nM, coupled with partial agonist activity at the 5-HT1F receptor, with an EC50 of 77.91 nM. This compound demonstrates significant efficacy in preclinical migraine models, effectively reducing the expression levels of CGRP and c-Fos proteins and inhibiting ERK and CREB phosphorylation. PCC0105005 is suitable for research focused on migraine pathophysiology and potential therapeutic interventions.
Out of stock
All 3 sizes
Calcitonin (8-32), salmon is a selective antagonist of the amylin receptor, primarily involved in the regulation of glucose homeostasis and appetite control. This peptide exhibits potent inhibitory effects on amylin signaling, making it a valuable tool for research into metabolic disorders and potential therapeutic approaches for conditions such as diabetes and obesity. Its specificity and functionality allow for detailed studies of amylin-related pathways in various biological contexts.
AC 187 is a potent and orally bioavailable antagonist of the amylin receptor, exhibiting an IC50 of 0.48 nM and a Ki of 0.275 nM. This compound demonstrates selectivity for the amylin receptor over calcitonin and CGRP receptors. AC 187 has been shown to possess neuroprotective effects, making it a valuable tool for research in neurodegenerative diseases and metabolic disorders.
Acetyl-Amylin (8-37) (human) is a selective antagonist of the amylin receptor. This peptide fragment inhibits amylin activity, providing valuable insights into its role in metabolic processes and glucose homeostasis. It is utilized in research addressing diabetes, obesity, and related cardiovascular conditions, contributing to the understanding of amylin signaling pathways and potential therapeutic interventions.
Out of stock
All 3 sizes
Synonyms: Zavegepant (hydrochloride); BHV-3500 (hydrochloride)
Vazegepant hydrochloride is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a high binding affinity with a Ki value of 0.023 nM. This compound represents the first intranasal formulation in the gepant class, specifically developed for the acute management of migraine. Additionally, Vazegepant hydrochloride shows potential in addressing pulmonary inflammation associated with COVID-19, enabling further research into its therapeutic applications in these areas.
Synonyms: MK-8031; AGN-241689
Atogepant is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting potent oral bioavailability. It is primarily utilized in research related to migraine pathophysiology and therapeutic interventions, contributing to the understanding of CGRP’s role in migraine mechanisms. This compound enables detailed investigations into migraine relief strategies targeting CGRP signaling pathways.
Synonyms: Zavegepant; BHV-3500
Vazegepant is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. It selectively inhibits the CGRP receptor, thereby modulating pain pathways associated with migraine. This compound is valuable for research on migraine treatments and the role of CGRP in nociceptive signaling.
Synonyms: BMS-927711 sulfate hydrate; BHV-3000 sulfate hydrate
Rimegepant sulfate hydrate is a potent, orally active, selective antagonist of the calcitonin gene-related peptide (CGRP) receptor. It exhibits a binding affinity with a Ki of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound is primarily utilized in migraine research, contributing to studies focused on novel therapeutic approaches for migraine management.
HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist that plays a significant role in the study of migraine pathology. It effectively inhibits CGRP receptor activity, which is critical for understanding migraine mechanisms and developing therapeutic strategies. HTL22562 is primarily used in acute research settings to explore the implications of CGRP signaling in headache disorders.
CGRP Antagonist 7 is a highly potent calcitonin gene-related peptide (CGRP) receptor antagonist, exhibiting a Ki value of 0.029 nM. This compound effectively inhibits the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP Antagonist 7 is primarily utilized in research focused on migraine pathophysiology and therapeutic interventions targeting CGRP signaling pathways.
Out of stock
All 3 sizes
MK-8825 is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating a Ki value of 47 pM for human and 17 nM for rat receptors. It effectively inhibits CGRP-mediated cAMP responses, showcasing competitive antagonism. This compound is valuable for research into migraine and temporomandibular joint disorders, contributing to the understanding of therapeutic targets in these conditions.
Synonyms: BMS-927711 hemisulfate; BHV-3000 hemisulfate
Rimegepant hemisulfate is a selective and competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor, exhibiting a Ki value of 0.027 nM and an IC50 of 0.14 nM for the human CGRP receptor. This compound demonstrates potent biological activity in blocking CGRP signaling pathways, making it a valuable tool for migraine research and the investigation of related neurological conditions. Its oral bioavailability supports its application in in vivo studies focused on migraines and CGRP-mediated mechanisms.
Out of stock
All 3 sizes
Desfluoro-BMS-694153 is a potent antagonist of the calcitonin gene-related peptide (CGRP) receptor, with a Ki value of 0.01 nM. This compound exhibits minimal risk of CYP3A4 inhibition, demonstrated by IC50 values of 36 μM for CYP3A4-BFC and 6 μM for CYP3A4-BZR. Desfluoro-BMS-694153 is primarily utilized in research focused on migraine pathophysiology and the exploration of therapeutic interventions targeting CGRP pathways.
Out of stock
All 3 sizes
BMS-846372 is a potent oral antagonist of the calcitonin gene-related peptide (CGRP), exhibiting a Ki value of 0.07 nM. This compound is primarily utilized in research studies focused on migraine pathophysiology and may aid in the development of therapeutic strategies for migraine management.
Out of stock
All 3 sizes