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-P10956
    Colulintide
    		Agonist 98.35%
    Colulintide (LY3541105) is an amylin-calcitonin dual receptor agonist with Amylin as its scaffold. Colulintide is applicable to research related to type 2 diabetes and obesity.
    Colulintide
  • HY-120294
    Chrysin 6-C-glucoside 8-C-arabinoside
    		98.55%
    Chrysin 6-C-glucoside 8-C-arabinoside can inhibit the CGRP releasing and the activation of TRPV1 channel. Chrysin 6-C-glucoside 8-C-arabinoside can be used for anti-migraine research.
    Chrysin 6-C-glucoside 8-C-arabinoside
  • HY-P1770
    Adrenomedullin (16-31), human
    		99.96%
    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.
    Adrenomedullin (16-31), human
  • HY-P11320
    Davalintide
    		Agonist 98.04%
    Davalintide is an Amylin (HY-P1464)-mimetic peptide with greater potency and longer-lasting effects. Davalintide is a potent agonist of amylin receptor (IC50 = 0.04 nM), calcitonin receptor (IC50 = 0.06 nM) and calcitonin related peptide receptor (CGRP receptor) (IC50 = 3.1 nM). Davalintide shows stronger potency to Amylin to activate cyclic AMP production through the calcitonin receptor (EC50 = 1.4 nM). Davalintide regulates blood sugar and weight through various mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and reducing food intake. Davalintide can be used for the studies of anti-obesity and anti-diabetes.
    Davalintide
  • HY-121300
    Kendomycin
    		Agonist 98.00%
    Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent.
    Kendomycin
  • 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-P3919A
    Adrenotensin (human) TFA
    		99.09%
    Adrenotensin (human) (Pro-ADM-153-185 (human)) TFA is a 153-185 fragment of precursor peptide of Adrenomedullin. Adrenomedullin (ADM) TFA is a 52-amino acid multifunctional peptide, which belongs to the CGRP superfamily of vasoactive peptide hormones.
    Adrenotensin (human) TFA
  • HY-W770410
    9-PAHSA-13C4
    		Agonist 99.9%
    9-PAHSA-13C4 is 13C-labeled 9-PAHSA. 9-PAHSAis an orally active endogenous GPR120 agonist (EC50=18 μM). 9-PAHSAsignificantly inhibits LPS-induced inflammatory responses by blocking the NF-κB pathway. 9-PAHSAinduces 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-PAHSAregulates 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-PAHSAdoes not directly regulate insulin secretion or improve systemic insulin sensitivity, and possesses specific anti-inflammatory, metabolic regulatory and neuroprotective properties. 9-PAHSAcan be used in the research of diabetes-related cognitive impairment, obesity and non-alcoholic fatty liver disease.
    9-PAHSA-<sup>13</sup>C<sub>4</sub>
  • 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-P990497
    Anti-RAMP3 Antibody
    		Inhibitor
    Anti-RAMP3 Antibody is a CHO expressed human antibody that targets RAMP3. The Anti-RAMP3 Antibody features a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-RAMP3 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-RAMP3 Antibody
  • HY-P0090S
    Calcitonin-13C6,15N4 (salmon) TFA
    		Agonist
    Calcitonin-13C6,15N4 (salmon) (Salmon calcitonin-13C6,15N4) TFA is 13C and 15N-labeled Calcitonin (salmon) (HY-P0090). Calcitonin (salmon) , a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
    Calcitonin-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N<sub>4</sub> (salmon) TFA
  • HY-P4863
    Biotinyl-Amylin (human)
    		Agonist
    Biotinyl-Amylin (human) is a biotin-labeled derivative of Amylin, amide, human (HY-P1070). Biotinyl-Amylin (human) acts as a competitive agonist for the Calcitonin Receptor (CTR) and for the Amylin receptors (AMY1, AMY2, and AMY3) formed by the association of CTR with RAMP1/2/3. By mimicking endogenous human amylin, Biotinyl-Amylin (human) binds to and activates CTR and AMY receptors, thereby initiating downstream signaling pathways involving cAMP, CREB, and ERK1/2, while retaining high-affinity receptor binding and activation capabilities. Biotinyl-Amylin (human) is primarily utilized in studies investigating the metabolic regulatory mechanisms underlying obesity and diabetes; it is also applicable to pharmacological research, receptor localization studies, and ligand-binding assays related to Amylin receptors in the context of Alzheimer's disease.
    Biotinyl-Amylin (human)
  • HY-144026S
    9-PAHSA-d9
    		Agonist
    9-PAHSA-d9 is the deuterium labeled 9-PAHSA (HY-120657). 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>9</sub>
  • HY-145353
    HTL22562
    		Antagonist
    HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute research of migraine.
    HTL22562
  • HY-186104
    AMYR/CTR agonist 1
    		Agonist
    AMYR/CTR agonist 1 (Compound 195) is a pancreatic amylin receptor and calcitonin receptor (AMYR/CTR) agonist with EC50 values for pancreatic amylin receptor and calcitonin receptor cAMP of 99.5 and 6.16 pM respectively. AMYR/CTR agonist 1 can be used in the research of diseases such as type 2 diabetes and obesity.
    AMYR/CTR agonist 1
  • 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-185229B
    rel-CTR/AMYR agonist-1
    		Agonist
    rel-CTR/AMYR agonist-1 (Example 169) is an agonist of amylin and/or calcitonin receptor.
    rel-CTR/AMYR agonist-1
  • 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
Cat. No. Product Name / Synonyms Application Reactivity