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.

CGRP Receptor Related Products (42):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant
    Antagonist 99.50%
    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 Ki of 14.4 pM for human CGRP.
  • HY-15498
    Rimegepant
    Antagonist 99.83%
    Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM and an IC50 of 0.14 nM for hCGRP receptor.
  • HY-P0209
    Rat CGRP-(8-37)
    Antagonist 99.28%
    Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
  • HY-P0203A
    α-CGRP, rat TFA
    98.94%
    α-CGRP, rat TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP, rat TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP, rat TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies.
  • HY-32709
    Telcagepant
    Antagonist 99.55%
    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.
  • HY-109022
    Atogepant
    Antagonist 99.90%
    Atogepant (MK-8031) is an orally active and selective calcitonin gene–related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
  • HY-P3462
    Cagrilintide
    Agonist
    Cagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake. Cagrilintide has the potential for the research of obesity.
  • HY-P3462A
    Cagrilintide acetate
    Agonist
    Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies.
  • HY-P1548A
    β-CGRP, human TFA
    99.10%
    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.
  • HY-P0090
    Calcitonin (salmon)
    Agonist 98.52%
    Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
  • HY-132131
    Vazegepant hydrochloride
    Antagonist 98.01%
    Vazegepant (BHV-3500) hydrochloride is a highly soluble CGRP receptor antagonist (hCGRP Ki= 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.
  • HY-10095A
    Olcegepant hydrochloride
    Antagonist 99.31%
    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 Ki of 14.4 pM for human CGRP.
  • HY-P1071A
    α-CGRP(human) TFA
    99.95%
    α-CGRP(human) TFA is a regulatory neuropeptide of 37 amino acids. α-CGRP(human) is widely distributed in the central and peripheral nervous system. α-CGRP(human) TFA is a potent vasodilator.
  • HY-P1071
    α-CGRP(human)
    99.76%
    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.
  • HY-12366
    Ubrogepant
    Antagonist 99.69%
    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
  • HY-10301
    MK-3207
    Antagonist 99.76%
    MK-3207 is an orally active, highly selective and species-specific CGRP receptor antagonist (for human CGRP receptor: IC50=0.12 nM; Ki=0.024 nM). MK-3207 can be used for migraine studies.
  • HY-P1471
    Adrenomedullin (AM) (22-52), human
    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.
  • HY-10302
    MK-3207 Hydrochloride
    Antagonist 99.06%
    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.
  • HY-P1014
    HCGRP-(8-37)
    Antagonist 98.0%
    HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
  • HY-P2273
    Calcitonin (human)
    Agonist
    Calcitonin (human) is a hypocalcemic hormone. Calcitonin can lower blood calcium levels and inhibit bone resorption. Calcitonin can be used in hypercalcemia or osteoporosis research.