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.

Cat. No. Product Name Effect Purity Chemical Structure
  • 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-120657S1
    9-PAHSA-d31
    Agonist 99.00%
    9-PAHSA-d31 is the deuterium labeled 9-PAHSA. 9-PAHSA is an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSA significantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSA induces adipocyte browning, enhances glucose uptake and reduces lipid accumulation, while improving mitochondrial function and the survival rate of steatotic hepatocytes. In terms of neuroprotection, 9-PAHSA regulates the expression of REST and BDNF in the prefrontal cortex of diabetic mice, and effectively prevents spatial working memory deficits and abnormal social behaviors. 9-PAHSA does not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSA can be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
    9-PAHSA-d<sub>31</sub>
  • 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
  • HY-185229
    CTR/AMYR agonist-1
    Agonist
    CTR/AMYR agonist-1 is a CTR/AMYR agonist with EC50 values of 0.56-6.9 nM. CTR/AMYR agonist-1 can be used for the research of metabolic disease.
    CTR/AMYR agonist-1
  • HY-179728
    Amylin agonist 1
    Agonist
    Amylin agonist 1 (Example 239a) is a receptor 3 for pancreatic amyloid peptide (bAMY3R) agonist, and its EC50 for stimulating cAMP production in cells is 6.17 nM. Amylin agonist 1 is also a receptor for calcitonin (bCTR) agonist, with its EC50 being 8.58 nM. Amylin agonist 1 can be used for research on type 2 diabetes and obesity.
    Amylin agonist 1
Cat. No. Product Name / Synonyms Application Reactivity