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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Davalintide
0 ImagesDavalintide 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.
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Kendomycin
0 ImagesCat. No.: HY-121300CAS No.: 183202-73-5Synonyms: (-)-TAN2162Kendomycin ((−)-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.
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Vazegepant hydrochloride
0 ImagesSynonyms: Zavegepant hydrochloride; BHV-3500 hydrochlorideVazegepant (Zavegepant hydrochloride; BHV-3500 hydrochloride) hydrochloride is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 23 pM for human CGRP receptor and an EC50 of 880 pM for reversing CGRP-induced vasodilation in human intracranial arteries. Vazegepant hydrochloride can block CGRP-mediated vasodilation in the trigeminal vascular system and inhibit neuronal circuit sensitization. Vazegepant hydrochloride can be used in migraine-related research.
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CTR/AMYR modulator-2
0 ImagesCat. No.: HY-185107CAS No.: 3108095-52-6CTR/AMYR modulator-2 is a dual agonist of human amylin receptor 3 (AMY3R) and calcitonin receptor (CTR). CTR/AMYR modulator-2 activates AMY3R and CTR, stimulating Rel EC50 of cAMP production in UMUC3 cells by 4 nM and 1 nM, respectively. CTR/AMYR modulator-2 may be used in research on type 2 diabetes and obesity.
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CGRP antagonist 1
0 ImagesCGRP 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.
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KBP-089
0 ImagesKBP-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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CGRP antagonist 2
0 ImagesCGRP antagonist 2 is a CGRP antagonist. CGRP antagonist 2 can be used in research on visceral pain and gastrointestinal disorders (such as functional bowel disorders and inflammatory bowel disease).
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Adrenotensin (human) TFA
0 ImagesCat. No.: HY-P3919APurity: 99.09%Synonyms: Pro-ADM-153-185 (human) TFAAdrenotensin (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.
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9-PAHSA-13C4
0 Images9-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.
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MK-3207 hydrochloride (Standard)
0 ImagesCat. No.: HY-10302RCAS No.: 957116-20-0MK-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.
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Anti-RAMP3 Antibody
0 ImagesCat. No.: HY-P990497Anti-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).
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Calcitonin-13C6,15N4 (salmon) TFA
0 ImagesCat. No.: HY-P0090SSynonyms: Salmon calcitonin-13C6,15N4 TFACalcitonin-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.
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Biotinyl-Amylin (human)
0 ImagesBiotinyl-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.
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9-PAHSA-d9
0 ImagesCat. No.: HY-144026SCAS No.: 1809222-43-29-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.
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HTL22562
0 ImagesCat. No.: HY-145353CAS No.: 2097085-63-5HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute research of migraine.
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Rimegepant-d4
0 ImagesCat. No.: HY-15498SSynonyms: BMS-927711-d4; BHV-3000-d4Rimegepant-d4 (BMS-927711-d4) is the deuterium labeled Rimegepant (HY-15498). Rimegepant (BMS-927711) 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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AMYR/CTR agonist 1
0 ImagesCat. No.: HY-186104CAS No.: 3097592-82-7AMYR/CTR agonist 1 is an amylin receptor (AMYR) and calcitonin receptor (CTR) agonist with an amylin receptor cAMP stimulation EC50 of 0.0995 nM and a calcitonin receptor cAMP stimulation EC50 of 0.00616 nM. AMYR/CTR agonist 1 can be used for the research of non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, insulin dependent diabetes, non-insulin dependent diabetes, impaired glucose tolerance, obesity, syndrome x.
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CGRP antagonist 7
0 ImagesCat. No.: HY-174986CAS No.: 2173508-07-9CGRP 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.
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rel-CTR/AMYR agonist-1
0 ImagesCat. No.: HY-185229BCAS No.: 3108096-13-2rel-CTR/AMYR agonist-1 is an agonist of amylin and/or calcitonin receptor. rel-CTR/AMYR agonist-1 can be used in research on metabolic diseases such as type 2 diabetes and obesity.
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MK-8825
0 ImagesCat. No.: HY-117694CAS No.: 1380887-60-4MK-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.
