1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. CGRP Receptor

CGRP Receptor

Calcitonin gene-related peptide receptor

CGRP receptor is a heterodimer formed by calcitonin-receptor-like receptor (CRLR), a type II (family B) G-protein-coupled receptor, and receptor-activity-modifying protein 1 (RAMP1), a single-membrane-pass protein. RAMP1 is needed for CGRP binding and also cell-surface expression of CLR. CLR is an example of a family B GPCR.

CGRP is a neuropeptide abundant in the trigeminal system and widely expressed in both the peripheral and central nervous systems. CGRP has several functions including vasodilation, the perception of painful stimuli, and inflammation. CGRP exerts its biological action by interacting with its receptors. There are two types of CGRP receptors, CGRP-A and CGRP-B.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19960
    BCTC
    Inhibitor 99.66%
    BCTC is an orally active current inhibitor of vanilloid receptor type 1 (VR1). BCTC is a transient receptor potential cation channel subfamily M member 8 (TRPM8) and transient receptor potential vanilloid 1 (TRPV1) antagonist. BCTC is an insulin sensitizer and secretor. BCTC has anticancer and analgesic effects.
    BCTC
  • HY-P0203B
    β-CGRP (mouse)
    99.77%
    β-CGRP (mouse) is a calcitonin gene-related peptide that induces vasodilation. β-CGRP (mouse) can be utilized in cardiovascular, pro-inflammatory, migraine and metabolic research.
    β-CGRP (mouse)
  • HY-P99021
    Galcanezumab
    Antagonist 98.00%
    Galcanezumab (LY 2951742) is a humanized IgG4 monoclonal antibody against the CGRP ligand. Galcanezumab can be used for migraine or cluster headaches research.
    Galcanezumab
  • HY-32709
    Telcagepant
    Antagonist 98.63%
    Telcagepant (MK-0974) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with Kis of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors, respectively.
    Telcagepant
  • HY-P9938
    Erenumab
    Inhibitor 98.88%
    Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine.
    Erenumab
  • HY-134992
    Vazegepant
    Antagonist 99.54%
    Vazegepant (Zavegepant) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist. Vazegepant can be used in the study of migraine.
    Vazegepant
  • HY-120657
    9-PAHSA
    Agonist 99.88%
    9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
    9-PAHSA
  • HY-P99017
    Eptinezumab
    Inhibitor 99.90%
    Eptinezumab (ALD-403) is a human monoclonal antibody targeting the α and β subtypes of human calcitonin gene-related peptide (CGRP). Eptinezumab binds to the CGRP ligand and blocks its binding to endogenous CGRP receptors, thereby inhibiting receptor activation. Eptinezumab can be used in research related to migraine.
    Eptinezumab
  • HY-P1548A
    β-CGRP, human TFA
    99.57%
    β-CGRP, human TFA (Human β-CGRP TFA) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells.
    β-CGRP, human TFA
  • HY-P1014
    HCGRP-(8-37)
    Antagonist 99.51%
    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.
    HCGRP-(8-37)
  • HY-P4058
    Calcitonin gene-related peptide free acid
    99.30%
    Calcitonin gene-related peptide (CGRP) free acid is a 37-amino acid neuropeptide, which represents the deamidated form of α-CGRP (human) (HY-P1071). Calcitonin gene-related peptide free acid is produced in the central and peripheral nervous systems of rats, and localizes to specific sensory, integrative and motor neuron systems, including those involved in nociception/thermoreception, feeding behavior, olfaction and visceral motor functions.
    Calcitonin gene-related peptide free acid
  • HY-P1071A
    α-CGRP (human) TFA
    98.12%
    α-CGRP (human) (TFA) is a regulatory neuropeptide of 37 amino acids. α-CGRP (human) (TFA) is widely distributed in the central and peripheral nervous system. α-CGRP (human) (TFA) is a potent vasodilator and has inotropic and chronotropic effects.
    α-CGRP (human) TFA
  • HY-103302
    SUN B8155
    Agonist 99.89%
    SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.
    SUN B8155
  • HY-P1913A
    Calcitonin Gene Related Peptide II (rat) TFA
    Activator 99.89%
    Calcitonin Gene Related Peptide II rat TFA, a CGRP receptor activator, is a potent and long-lasting vasodilator. Calcitonin Gene Related Peptide II rat TFA can be used in the research of cardiovascular diseases.
    Calcitonin Gene Related Peptide II (rat) TFA
  • HY-P1534
    Adrenomedullin (1-50), rat
    Activator 99.56%
    Adrenomedullin (1-50), rat is a 50 amino acid peptide, which induces a selective arterial vasodilation via activation of CGRP1 receptor.
    Adrenomedullin (1-50), rat
  • HY-10302
    MK-3207 Hydrochloride
    Antagonist 99.23%
    MK-3207 (Hydrochloride) is a potent and orally bioavailable CGRP receptor antagonist with IC50 of 0.12 nM and Ki of 0.024 nM, and is highly selective versus human AM1, AM2, CTR, and AMY3.
    MK-3207 Hydrochloride
  • HY-179738
    CTR/AMYR modulator-1
    Modulator 99.71%
    CTR/AMYR modulator-1 is a calcitonin receptor/amylin receptor modulator. CTR/AMYR modulator-1 can be used for the research of metabolic disease.
    CTR/AMYR modulator-1
  • HY-P3689
    [Tyr22] Calcitonin Gene Related Peptide, (22-37), rat
    Activator 99.86%
    [Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a fragments 22-37 of rat calcitonin gene related peptide (CGRP), targeting CGRP receptor and adenylate cyclase. Calcitonin is mainly produced by thyroid C cells while CGRP is secreted and stored in the nervous system.
    [Tyr22] Calcitonin Gene Related Peptide, (22-37), rat
  • HY-P1072
    PHM-27 (human)
    Agonist 99.09%
    PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
    PHM-27 (human)
  • HY-15498A
    Rimegepant sulfate hydrate
    Antagonist 99.56%
    Rimegepant (BMS-927711) sulfate hydrate is a potent, orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor. Rimegepant sulfate hydrate can be used for migraine research.
    Rimegepant sulfate hydrate
Cat. No. Product Name / Synonyms Application Reactivity