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CGRP Receptor antagonist
MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.- Marlene Dallmayer, .et al. , bioRxiv, 2018, 2018
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CGRP receptor antagonist
MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors. -
CGRP1 receptor
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. -
CGRP receptor antagonist
BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect. -
CGRP receptor antagonist
HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
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CGRP receptor antagonist
CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively. -
CGRP antagonist
Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine. -
CGRP1 receptor antagonist
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. - α-CGRP(human) is a regulatory neuropeptide of 37 amino acids. α-CGRP(human) is widely distributed in the central and peripheral nervous system. α-CGRP(human) is a potent vasodilator.
- Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
- 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.
- Calcitonin gene-related peptide (CGRP) free acid is a neuropeptide. Calcitonin gene-related peptide can be used for the research of nociception, ingestive behaviour and modulation of the endocrine systems.
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CGRP Receptor Antagonist/5-HT1F Receptor Agonist
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. -
Neuropeptide
α-CGRP (mouse, rat) is a neuropeptide that primarily targets the neuromuscular junction and functions as a potent vasodilator. It is known to induce a decrease in blood pressure and an increase in heart rate upon peripheral administration, and it also promotes relaxation of colonic smooth muscle. This peptide is valuable for research applications in cardiovascular studies, pro-inflammatory responses, migraine pathophysiology, and metabolic processes. -
CGRP Receptor Antagonist
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. -
Calcitonin Peptide
β-CGRP, human is a member of the calcitonin peptide family and functions through binding to the calcitonin-receptor-like receptor (CRLR) in conjunction with receptor-activity-modifying proteins (RAMPs). It exhibits high affinity, with IC50 values of 1 nM for the CRLR/RAMP1 complex and 300 nM for the CRLR/RAMP2 complex in cellular assays. This peptide is crucial for research in pain modulation, migraine mechanisms, and neurobiological studies. -
CGRP Antagonist
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. -
CGRP Receptor Antagonist
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. -
CGRP Receptor Activator
Adrenomedullin (1-50), rat is a 50 amino acid peptide that functions as a CGRP receptor activator. It is known to induce selective arterial vasodilation, making it relevant for research in cardiovascular physiology and pathophysiology. This peptide is utilized in studies investigating the role of adrenomedullin in vascular regulation and its potential therapeutic applications in hypertension and related disorders. -
CGRP Receptor Antagonist
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. -
hADM Analog
Adrenomedullin (16-31), human is a peptide fragment comprising amino acid residues 16-31 of human adrenomedullin (hADM). This analog exhibits significant affinity for the CGRP1 receptor, influencing cardiovascular regulation. It has been shown to elicit pressor activity in the systemic vascular bed of rats, making it a valuable tool for exploring vascular responses and related research applications. -
CGRP Receptor Antagonist
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
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. -
CGRP Receptor Antagonist
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. -
CGRP Receptor Antagonist
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. -
CGRP Receptor Antagonist
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. -
Fragment of Pro-Adrenomedullin
Adrenotensin (human), a fragment of pro-adrenomedullin, corresponds to amino acids 153-185 of the precursor peptide. As a member of the calcitonin gene-related peptide (CGRP) superfamily, Adrenomedullin (ADM) functions as a multifunctional vasoactive hormone. This fragment is relevant for research applications targeting cardiovascular physiology, cellular signaling, and pathophysiological processes associated with ADM. -
CGRP Antagonist
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. -
CGRP Antagonist
CGRP Antagonist 2 is a competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor. It effectively inhibits CGRP-mediated signaling, which is crucial for the modulation of nociceptive pathways associated with pain perception. This reagent is widely utilized in research focused on migraine mechanisms and pain management therapies. -
CGRP Receptor Activator
Calcitonin Gene Related Peptide II (rat) is a CGRP receptor activator that functions as a potent and enduring vasodilator. It plays a crucial role in the regulation of vascular tone and blood pressure. This peptide is utilized in research on cardiovascular diseases, aiding in the exploration of therapeutic strategies for conditions such as hypertension and vascular dysfunction. -
CGRP Receptor Agonist
Calcitonin (salmon) (acetate) functions as a calcitonin gene-related peptide (CGRP) receptor agonist. This compound stimulates bone formation while inhibiting bone resorption, making it valuable for research in osteoporosis and other bone-related disorders. The acetate form enhances the absorption and bioactivity of the peptide, providing a more effective hormonal intervention for studies focusing on bone metabolism and calcium homeostasis. -
Active Compound
Adrenomedullin (11-50), rat is a bioactive peptide fragment that represents the C-terminal portion of rat adrenomedullin. This compound primarily targets CGRP1 receptors, effectively inducing selective arterial vasodilation. Its key biological activity makes it useful in cardiovascular research, particularly in studies focusing on vascular function and regulation. -
CGRP Receptor Antagonist
BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP receptor). This compound exhibits significant biological activity in blocking CGRP-mediated signaling pathways, making it a valuable tool for migraine research. It is particularly effective in studies examining intranasal delivery methods for rapid therapeutic intervention in migraine treatment. -
Stable Isotope
Telcagepant-d8 is a deuterium-labeled variant of Telcagepant, a potent orally active antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits binding affinities (Kis) of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively. Telcagepant-d8 is primarily utilized in pharmacokinetic studies and metabolic research, providing a valuable tool for investigating CGRP-related pathways and receptor interactions in various biological systems. -
Amylin Receptor Antagonist
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. -
Amylin Receptor/Calcitonin Receptor/CGRP Receptor Agonit
Davalintide is a potent agonist of the amylin receptor, calcitonin receptor, and calcitonin gene-related peptide (CGRP) receptor, demonstrating high affinity with IC50 values of 0.04 nM, 0.06 nM, and 3.1 nM, respectively. It effectively stimulates cyclic AMP production via the calcitonin receptor, with an EC50 of 1.4 nM. Davalintide has been shown to regulate blood glucose levels and body weight through mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and suppressing food intake. This peptide is valuable for research applications focused on obesity and diabetes management. -
CGRP Agnalogue
[Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a CGRP analogue that targets the CGRP receptor and modulates adenylate cyclase activity. This peptide fragment, derived from the rat CGRP sequence, exhibits key biological activities associated with pain modulation and vasodilation. It is suitable for research applications studying neurogenic inflammation, cardiovascular regulation, and the pathophysiology of migraine headaches. -
TRPA1 Channel Antagonist
ADM 12 is a selective antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. It effectively inhibits nitroglycerin-induced trigeminal hyperalgesia in animal models, leading to decreased expression of pain-related genes such as c-Fos and TRPA1, as well as neuropeptides including CGRP and substance P. This compound holds potential for research applications in the fields of migraine and neuropathic pain. -
P/Q Type Ca2+ Channel Blocker
ω-Agatoxin IVA is a highly selective blocker of P/Q type calcium channels (Cav2.1), with IC50 values of 2 nM and 90 nM. This compound effectively inhibits glutamate exocytosis and calcium influx triggered by elevated potassium levels. Additionally, ω-Agatoxin IVA suppresses capsaicin-induced CGRP release and associated vasodilation. It is valuable for investigations into neurological and cardiovascular diseases, contributing to the understanding of calcium channel modulation in these contexts. -
CGRP Antagonist
SB 268262 is a selective antagonist of the calcitonin gene-related peptide (CGRP) receptor. This compound exhibits high affinity for CGRP receptors in the human brain, making it a valuable tool for studying CGRP signaling pathways. SB 268262 is applicable in research investigating the pharmacological properties of non-peptide CGRP receptor antagonists, also known as gepants, in models including rat, pig, and human meninges.

