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

CGRP Receptor

CGRP receptor is a heterotrimer: a large peptide with 7 transmembrane domains, named calcitonin receptor-like receptor (CLR or CRLR), is supplemented by a small single transmembrane peptide, named receptor activity-modifying protein (RAMP1) that forms the CGRP-specific ligand binding site. CGRP receptors are expressed by multiple different cell types within the nervous, cardiovascular and immune systems that are thought to play important roles in migraine pathology: on cerebral vascular smooth muscle, where they cause vasodilation, on dural mast cells triggering their degranulation, at the central terminals of the trigeminal nerve, where CGRP is a neuromodulator at second-order nociceptive neurons in the spinal trigeminal nucleus caudalis and in the dorsal horn of the spinal cord, where CGRP has a similar role in inducing central sensitisation to tactile stimuli. CGRP is produced in both peripheral and central neurons. It is a potent peptide vasodilator and can function in the transmission of pain.

CGRP Receptor Related Products (18):

Cat. No. Product Name Effect Purity
  • HY-10095
    Olcegepant Antagonist 99.32%
    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.
  • HY-32709
    Telcagepant Antagonist 99.07%
    Telcagepant (MK-0974) is a 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-10302
    MK-3207 Hydrochloride Antagonist 98.07%
    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-15498
    Rimegepant Antagonist 99.08%
    Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki value of 0.027 nM.
  • HY-10095A
    Olcegepant hydrochloride Antagonist 99.31%
    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.
  • HY-P1548A
    β-CGRP, human TFA 98.82%
    β-CGRP, human 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-P1766
    Adrenomedullin (11-50), rat Activator
    Adrenomedullin (11-50), rat is the C-terminal fragment (11-50) of rat adrenomedullin. Rat adrenomedullin induces a selective arterial vasodilation via CGRP1 receptors.
  • HY-P1770
    Adrenomedullin (16-31), human
    Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
  • HY-P1014
    HCGRP-(8-37) Antagonist 98.28%
    HCGRP-(8-37) is a human calcitonin gene-related peptide (hCGRP) fragment and also an antagonist of CGRP receptor.
  • HY-P0209
    Rat CGRP-(8-37) Antagonist 98.29%
    Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
  • HY-P1462A
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat TFA Modulator
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat (TFA) is a 37 amino acid calcitonin family of neuropeptide, acts through calcitonin receptor-like receptor (CRLR).
  • HY-P1548
    β-CGRP, human
    β-CGRP, human 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-10301
    MK-3207 Antagonist 98.76%
    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.
  • HY-P1471
    Adrenomedullin (AM) (22-52), human Antagonist
    Adrenomedullin (AM) (22-52), human is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
  • HY-112262
    CGRP antagonist 1 Antagonist
    CGRP antagonist 1 is a highly potent CGRP receptor antagonist with a Ki and IC50 of 35 and 57 nM, respectively.
  • HY-P1534
    Adrenomedullin (1-50), rat Activator
    Adrenomedullin (1-50), rat is a 50 amino acid peptide, which induces a selective arterial vasodilation via activation of CGRP1 receptor.
  • HY-P1462
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat Agonist
    Calcitonin Gene Related Peptide (CGRP) (83-119), rat is a 37 amino acid calcitonin family of neuropeptide, acts through calcitonin receptor-like receptor (CRLR).
  • HY-12366
    Ubrogepant Antagonist
    Ubrogepant (MK-1602) is a novel oral calcitonin gene-related peptide receptor (CGRP) antagonist in development for acute treatment of migraine.
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