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

CGRP Receptor

Calcitonin gene-related peptide receptor

CGRP Receptor

Related Products

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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. Product Name Effect Purity Chemical Structure
  • HY-174986
    CGRP antagonist 7
    		Antagonist
    CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine.
    CGRP antagonist 7
  • HY-117694
    MK-8825
    		Antagonist
    MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders.
    MK-8825
  • HY-15498B
    Rimegepant hemisulfate
    		Antagonist
    Rimegepant (BMS-927711) hemisulfate 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 hemisulfate can be used for migraine research.
    Rimegepant hemisulfate
  • 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.
    Adrenomedullin (AM) (22-52), human TFA
  • HY-180955
    Desfluoro-BMS-694153
    		Antagonist
    Desfluoro-BMS-694153 (Compound 3) is a calcitonin gene-related peptide receptor (CGRP receptor) antagonist, with a Ki value of 0.01 nM. Desfluoro-BMS-694153 has a significantly reduced risk of CYP3A4 inhibition, and its IC50 values for CYP3A4-BFC and CYP3A4-BZR are 36 and 6 μM respectively. Desfluoro-BMS-694153 can be used for research on migraines.
    Desfluoro-BMS-694153
  • HY-109022A
    (3R,5R,6S)-Atogepant
    		Antagonist 99.55%
    (3R,5R,6S)-Atogepant ((3R,5R,6S)-MK-8031) is the enantiomer of Atogepant (HY-109022). Atogepant is a calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
    (3R,5R,6S)-Atogepant
  • HY-12367
    BMS-846372
    		Antagonist
    BMS-846372 (Compound 5) is an orally active CGRP antagonist (Ki = 0.07 nM). BMS-846372 may be used in migraine research.
    BMS-846372
  • HY-109022S
    Atogepant-d4
    		Antagonist
    Atogepant-d4 (MK-8031-d4) is the deuterium labeled Atogepant (HY-109022). Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
    Atogepant-d<sub>4</sub>
  • HY-162925
    CGRP antagonist 6
    		Antagonist
    CGRP antagonist 6 (Compound 23) is a CGRP receptor antagonist (Ki: 0.84 nM). CGRP antagonist 6 can be used for research of migraine.
    CGRP antagonist 6
  • HY-P11769
    RM2
    		Antagonist
    RM2 is a GRPr antagonist. RM2 selectively binds to GRPr, blocks agonist-induced receptor internalization, and inhibits agonist-triggered intracellular calcium mobilization. RM2 can be used in studies related to prostate cancer.
    RM2
  • HY-179684
    PCC0105005
    		Antagonist
    PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine.
    PCC0105005
  • HY-114574
    BMS-694153
    		Antagonist
    BMS-694153 is a potent antagonist of the human calcitonin gene-related peptide receptor (CGRP Receptor). BMS-694153 can be used for migraine with rapid and efficient intranasal exposure.
    BMS-694153
  • HY-183181
    CGRP antagonist-9
    		Antagonist
    CGRP antagonist-9 is a CGRP receptor antagonist with an IC50 of 25 nM. It regulates the cAMP signaling pathway and can be used in migraine-related studies.
    CGRP antagonist-9
  • HY-12366R
    Ubrogepant (Standard)
    		Antagonist
    Ubrogepant (Standard) is the analytical standard of Ubrogepant. This product is intended for research and analytical applications. 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 (Standard)
  • 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.
    Ubrogepant-d<sub>5</sub>
  • HY-183142
    CLR/RAMP3-receptor antagonist-1
    		Antagonist
    CLR/RAMP3-receptor antagonist-1 is a selective antagonist of the CLR/RAMP3 receptor (CLR/RAMP3, AM2 receptor), with pIC50 values of 5.86, 9.21 and 9.07 against AM1 (CLR/RAMP2), AM2 (CLR/RAMP3) and CGRP (CLR/RAMP1) receptors, respectively. CLR/RAMP3-receptor antagonist-1 reduces the levels of pancreatic cancer progression markers, induces apoptosis in vitro, and prolongs survival in mouse models of pancreatic cancer. CLR/RAMP3-receptor antagonist-1 can be used in pancreatic cancer-related research.
    CLR/RAMP3-receptor antagonist-1
  • HY-109022R
    Atogepant (Standard)
    		Antagonist
    Atogepant (Standard) is the analytical standard of Atogepant (HY-109022). This product is intended for research and analytical applications. Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine.
    Atogepant (Standard)
  • HY-10095R
    Olcegepant (Standard)
    		Antagonist
    Olcegepant (Standard) is the analytical standard of Olcegepant (HY-10095). This product is intended for research and analytical applications. 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 (Standard)
  • 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.
    Telcagepant-d<sub>8</sub>
  • HY-183180
    CGRP antagonist-8
    		Antagonist
    CGRP antagonist-8 is a CGRP receptor antagonist with an IC50 of 2.7 nM. CGRP antagonist-8 can be used for the research of migraine.
    CGRP antagonist-8
Cat. No. Product Name / Synonyms Application Reactivity