- Signaling Pathways
- GPCR/G Protein Neuronal Signaling
- 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.
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CGRP Receptor Related Products (106)
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Antibodies (1)
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Cagrilintide
0 ImagesCagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake. Cagrilintide has the potential for the research of obesity. -
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Olcegepant
0 ImagesSynonyms: BIBN-4096; BIBN 4096BSOlcegepant (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. -
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α-CGRP (human)
0 ImagesSynonyms: Calcitonin gene-related peptideα-CGRP (human) (Calcitonin gene-related peptide) is a regulatory neuropeptide of 37 amino acids. α-CGRP (human) is widely distributed in the central and peripheral nervous system. α-CGRP (human) is a potent vasodilator and has inotropic and chronotropic effects. -
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α-CGRP (mouse, rat)
0 ImagesSynonyms: CGRP (83-119), mouse, ratα-CGRP (mouse, rat), a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, rat) can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP (mouse, rat) has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies. -
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Calcitonin (salmon)
0 ImagesSynonyms: Salmon calcitoninCalcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption. -
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Vazegepant hydrochloride
0 ImagesSynonyms: Zavegepant hydrochloride; BHV-3500 hydrochlorideVazegepant (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. -
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CTR/AMYR modulator-2
0 ImagesCat. No.: HY-185107CAS No.: 3108095-52-6CTR/AMYR modulator-2 (Example 107) is a receptor 3 for pancreatic amyloid peptide (bAMY3R) agonist, and its EC50 for stimulating cAMP production in cells is <500 nM. CTR/AMYR modulator-2 is also a receptor for calcitonin (bCTR) agonist, with its EC50 being <5000 nM. CTR/AMYR modulator-2 can be used for research on type 2 diabetes and obesity. -
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KBP-089
0 ImagesCat. No.: HY-P11610CAS No.: 1776112-67-4KBP-089 is a dual Amylin and Calcitonin Receptor agonist. KBP-089 reduces body weight, decreases adipose tissue mass and improves glucose tolerance in obese rats. KBP-089 also eliminates lipid accumulation in the liver and muscle, and ameliorates glycemic homeostasis and insulin sensitivity. KBP-089 is applicable to the research of diseases such as obesity and type 2 diabetes. -
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Rimegepant
0 ImagesSynonyms: BMS-927711; BHV-3000Rimegepant (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 . -
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Cagrilintide acetate
0 ImagesCat. No.: HY-P3462APurity: 99.96%Cagrilintide acetate is a non-selective AMYR/CTR agonist and long-acting acylated amylase analogue. Cagrilintide acetate causes a reduction in food intake and significant weight loss in a dose-dependent manner. Cagrilintide acetate can be used in obesity studies. -
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Calcitonin (human)
0 ImagesCalcitonin (human) is a hypocalcemic hormone. Calcitonin can lower blood calcium levels and inhibit bone resorption. Calcitonin can be used in hypercalcemia or osteoporosis research. -
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Adrenomedullin (AM) (22-52), human
0 ImagesSynonyms: 22-52-Adrenomedullin (human)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. -
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Rat CGRP-(8-37)
0 ImagesRat CGRP-(8-37) (VTHRLAGLLSRSGGVVKDNFVPTNVGSEAF) is a highly selective CGRP receptor antagonist. -
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α-CGRP (mouse, rat) TFA
0 ImagesCat. No.: HY-P0203APurity: 99.82%Synonyms: CGRP (83-119), mouse, rat TFAα-CGRP (mouse, rat) TFA, a neuropeptide (calcitonin gene-related peptide (CGRP)) mainly expressed in neuromuscular junction, is a potent vasodilator. α-CGRP (mouse, rat) TFA can lead to a fall in blood pressure and an increase in heart rate by peripheral administration, also relax colonie smooth muscle. α-CGRP (mouse, rat) TFA has the potential in cardiovascular, pro-inflammatory, migraine and metabolic studies. -
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β-CGRP, human
0 ImagesSynonyms: Human β-CGRP; CGRP-II (Human)β-CGRP, human (Human β-CGRP) is one of calcitonin peptides, acts via the complex of calcitonin-receptor-like receptor (CRLR) and receptor-activity-modifying protein (RAMP), with IC50s of 1 nM and 300 nM for CRLR/RAMP1 and CRLR/RAMP2 in cells. -
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Olcegepant hydrochloride
0 ImagesSynonyms: BIBN-4096 hydrochloride; BIBN4096BS hydrochlorideOlcegepant 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. -
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MK-3207
0 ImagesMK-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. -
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Atogepant
0 ImagesSynonyms: MK-8031; AGN-241689Atogepant (MK-8031) is an orally active and selective calcitonin gene-related peptide receptor (CGRP) antagonist. Atogepant can be used for researching migraine. -
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Fremanezumab
0 ImagesCat. No.: HY-P99019CAS No.: 1655501-53-3Synonyms: TEV-48125; LBR-101; PF-04427429; RN-307Fremanezumab (TEV-48125) is a humanized lgG2 monoclonal antibody that selectively and potently binds to calcitonin gene related peptide (CGRp) (IC50 values = 7.943 nM). Fremanezumab binds to mouse CGRP with an IC50 value of 19.6 nM. Fremanezumab counteracts anti-inflammatory effects of CGRP in vitro, including CGRP-mediated inhibition of LPS (HY-D1056)-induced microglial activation. Fremanezumab selectively inhibits the activation of Aδ meningeal nociceptors by cortical spreading depression (CSD) in rats. Fremanezumab can be used for the study of inflammation and chronic migraine. -
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BCTC
0 ImagesBCTC 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. -
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