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. 상품명 효과 Purity Chemical Structure
  • HY-P11587
    BGM1812
    Agonist
    BGM1812 is a dual agonist of amylin (hAMY3R) (EC50 = 0.627 nM) and CGRP Receptor (hCTR) (EC50 = 2.27 nM). BGM1812 achieves weight loss, increases the proportion of lean body mass, and reduces fat mass in diet-induced obese (DIO) rats. BGM1812 is applicable to research related to obesity.
    BGM1812
  • 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-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.
    Adrenomedullin (11-50), rat
  • HY-P11588
    KBP-042
    Activator
    KBP-042 is an orally active amylin receptor activator, a calcitonin receptor activator. KBP-042 induces sustained weight loss, reduces adipose tissue mass, lowers hepatic lipid deposition, increases plasma adiponectin, decreases plasma leptin, and reduces plasma glucose-dependent insulinotropic peptide levels. KBP-042 can be used for the research of obesity and insulin resistance.
    KBP-042
  • 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-P11629
    KBP-336
    Agonist
    KBP-336 is a dual amylin and calcitonin receptor agonist (DACRA). KBP-336 exhibits antidiabetic and insulin-sensitizing properties, improves glucose levels, spatial learning, and memory in diabetic rats, and reduces blood glucose. KBP-336 also alleviates pain-like symptoms in osteoarthritis rats. KBP-336 also promotes weight and fat reduction. KBP-336 is useful for research on diabetes, obesity, and arthritis.
    KBP-336
  • HY-119864
    Drinidene
    Inhibitor
    Drinidene can be used for the research of pain disorders extracted from patent AU2018254530A1.
    Drinidene
  • HY-19960R
    BCTC (Standard)
    Inhibitor
    BCTC (Standard) is the analytical standard of BCTC. This product is intended for research and analytical applications. 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.
    BCTC (Standard)
  • HY-185229A
    CTR/AMYR agonist-1 enantiomer
    Agonist
    CTR/AMYR agonist-1 enantiomer is an enantiomer of CTR/AMYR agonist-1 (HY-185229). 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 enantiomer
  • 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-103302R
    SUN B8155 (Standard)
    Agonist
    SUN B8155 (Standard) is the analytical standard of SUN B8155 (HY-103302). This product is intended for research and analytical applications. SUN B8155, a non-peptide agonist of calcitonin (CT) receptor, selectively mimics the biological actions of calcitonin. Calcitonin, a 32-amino acid peptide hormone secreted mainly from the thyroid gland, plays an important role in maintaining bone homeostasis.
    SUN B8155 (Standard)
  • 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-120657S
    9-PAHSA-d4
    Agonist
    9-PAHSA-d4 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>4</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-185234
    CTR/AMYR activator-1
    Activator
    CTR/AMYR activator-1 (S configuration of compound 122) is a CTR/AMYR activator. CTR/AMYR activator-1 can be used in the research of bone diseases, metabolic diseases, cardiovascular diseases, and neurodegenerative diseases.
    CTR/AMYR activator-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-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>
Cat. No. 상품명 / Synonyms Application Reactivity