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 (111)
Related Products (111)
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Antibodies (1)
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9-PAHSA-d4
0 ImagesCat. No.: HY-120657SCAS No.: 2704278-85-19-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.
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CLR/RAMP3-receptor antagonist-1
0 ImagesCat. No.: HY-183142CAS No.: 2252341-45-8CLR/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.
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CTR/AMYR activator-1
0 ImagesCat. No.: HY-185234CAS No.: 3068779-36-9CTR/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.
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Atogepant (Standard)
0 ImagesCat. No.: HY-109022RCAS No.: 1374248-81-3Synonyms: MK-8031 (Standard); AGN-241689 (Standard)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.
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Rimegepant (Standard)
0 ImagesCat. No.: HY-15498RCAS No.: 1289023-67-1Synonyms: BMS-927711 (Standard); BHV-3000 (Standard)Rimegepant (Standard) is the analytical standard of Rimegepant (HY-15498). This product is intended for research and analytical applications. Rimegepant (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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Olcegepant (Standard)
0 ImagesCat. No.: HY-10095RCAS No.: 204697-65-4Synonyms: BIBN-4096 (Standard); BIBN 4096BS (Standard)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.
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9-PAHSA-d31
0 ImagesCat. No.: HY-120657S1CAS No.: 2748208-06-09-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.
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Telcagepant-d8
0 ImagesCat. No.: HY-32709SCAS No.: 1132641-75-8Synonyms: MK-0974-d8Telcagepant-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.
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CGRP antagonist-8
0 ImagesCat. No.: HY-183180CAS No.: 1610413-85-8CGRP 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.
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CTR/AMYR agonist-2
0 ImagesCat. No.: HY-187461CAS No.: 3138389-44-0CTR/AMYR agonist-2 is a fused heterocyclic amide/sulfonamide compound, as well as a calcitonin G protein-coupled receptor (CGRP Receptor) / amylin receptor agonist. CTR/AMYR agonist-2 shows potential for application in research related to diseases such as obesity and type 2 diabetes.
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CTR/AMYR agonist-1
0 ImagesCat. No.: HY-185229CAS No.: 3108097-26-0CTR/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.
