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

CGRP 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 (60):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant Antagonist 99.83%
    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[1][2].
  • HY-P1071
    α-CGRP(human) 99.87%
    α-CGRP(human) (Calcitonin gene-related peptide) 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 and has inotropic and chronotropic effects[1][2][3].
  • HY-P0090
    Calcitonin (salmon) Agonist 99.95%
    Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
  • HY-P0203A
    α-CGRP (mouse, rat) (TFA) 99.29%
    α-CGRP (mouse, rat) TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, 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 (mouse, rat) TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies[1][2][3][4].
  • HY-P3462A
    Cagrilintide acetate Agonist 99.94%
    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[1][2][3].
  • HY-12366S
    Ubrogepant-d5 Antagonist
    Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. 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[1][2][3].
  • HY-15498A
    Rimegepant sulfate hydrate Antagonist
    Rimegepant (sulfate hydrate) is an orally active, selective and competitive calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 0.027 nM. Rimegepant (sulfate hydrate) can be used in migraine related research[1].
  • HY-32709S
    Telcagepant-d8 Antagonist
    Telcagepant-d8 (MK-0974-d8) is deuterium labeled Telcagepant. 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-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[1].
  • HY-P1548
    β-CGRP, human 98.17%
    β-CGRP, human (Human β-CGRP) 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[1].
  • 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[1][2][3][4][5].
  • HY-117694
    MK-8825 Antagonist
    MK-8825 is an orally active, potent and selective CGRP receptor antagonist, which shows concentration-dependent inhibition of Capsaicin (HY-10448)-evoked dermal blood flow with an EC50 value of about 7.4 μM. MK-8825 inhibits CGRP-induced spontaneous nociceptive facial grooming behaviors, neuronal activation in the trigeminal nucleus, and systemic release of pro-inflammatory cytokines in a mouse model of acute orofacial masseteric muscle pain. MK-8825 is promising for research of acute migraine[1][2].
  • HY-10095A
    Olcegepant hydrochloride Antagonist 99.39%
    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[1][2].
  • HY-P1471
    Adrenomedullin (AM) (22-52), human Antagonist 99.61%
    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[1][2].
  • HY-P99017
    Eptinezumab Inhibitor 99.90%
    Eptinezumab is a humanized monoclonal antibody. Eptinezumab binds to calcitonin gene-related peptide (CGRP) and blocks its interaction with the receptor. Eptinezumab can be used in the study of preventing migraines[1][2].
  • HY-P1471A
    Adrenomedullin (AM) (22-52), human TFA Antagonist
    Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat[1].
  • HY-121300
    Kendomycin Agonist 98.00%
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent[1][2].
  • HY-P1071A
    α-CGRP(human) TFA 98.44%
    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[1].
  • HY-P2601A
    Tyr-α-CGRP (human) TFA
    Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM[1][2].
  • HY-P99019
    Fremanezumab Inhibitor
    Fremanezumab (TEV-48125) is a humanized IgG2a monoclonal antibody that selectively and potently binds to calcitonin gene-related peptide (CGRP). CGRP is a 37-amino acid neuropeptide involved in central and peripheral pathophysiological events of migraine. Fremanezumab has the potential for chronic migraine research[1].