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

CGRP Receptor

Calcitonin gene-related peptide receptor

CGRP Receptor

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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. 상품명 효과 Purity Chemical Structure
  • 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.
    Olcegepant
  • HY-132131
    Vazegepant hydrochloride
    		Antagonist 99.36%
    Vazegepant (BHV-3500) hydrochloride is a highly affinity 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.
    Vazegepant hydrochloride
  • HY-15498S
    Rimegepant-d4
    		Antagonist
    Rimegepant-d4 (BMS-927711-d4) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine.
    Rimegepant-d<sub>4</sub>
  • HY-15498
    Rimegepant
    		Antagonist 99.99%
    Rimegepant (BMS-927711; BHV-3000) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
    Rimegepant
  • 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.
    Adrenomedullin (AM) (22-52), human
  • HY-P0209
    Rat CGRP-(8-37)
    		Antagonist 99.57%
    Rat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist.
    Rat CGRP-(8-37)
  • 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.
    Olcegepant hydrochloride
  • HY-10301
    MK-3207
    		Antagonist 99.60%
    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.
    MK-3207
  • HY-109022
    Atogepant
    		Antagonist 99.93%
    Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
    Atogepant
  • HY-12366
    Ubrogepant
    		Antagonist 99.90%
    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.
    Ubrogepant
  • 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-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-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-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-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
  • HY-112262
    CGRP antagonist 1
    		Antagonist 99.68%
    CGRP antagonist 1 (compound 21) is a highly potent CGRP receptor antagonist with a Ki and an IC50 of 1.7 nM and 5.7 nM, respectively.
    CGRP antagonist 1
  • HY-114945
    CGRP antagonist 2
    		Antagonist 99.75%
    CGRP antagonist 2 is a CGRP receptor antagonist. CGRP antagonist 2 can be used for pain relief.
    CGRP antagonist 2
  • HY-10302R
    MK-3207 hydrochloride (Standard)
    		Antagonist
    MK-3207 hydrochloride (Standard) is the analytical standard of MK-3207 hydrochloride (HY-10302). This product is intended for research and analytical applications. 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 (Standard)
  • HY-145353
    HTL22562
    		Antagonist
    HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute research of migraine.
    HTL22562
Cat. No. 상품명 / Synonyms Application Reactivity