Chemerin Receptor
Chemerin Receptor
Chemerin receptors are a type of membrane receptors that can specifically bind to chemerin and belong to the G-protein-coupled receptor family Class A. Currently, the main chemerin receptors include chemerin receptor 1, also known as ChemR23 or CMKLR1, and chemerin receptor 2, also known as GPR1. After chemerin binds to its receptor, it can recruit and activate immune cells, enhancing the body's innate and adaptive immune responses. At the same time, it can also regulate the functions of vascular endothelial cells and promote angiogenesis. Chemerin receptors are also involved in the regulation of energy metabolism and adipose tissue. Abnormalities in the expression and function of chemerin and its receptors are closely related to cancer, inflammatory diseases, and metabolic diseases such as obesity and diabetes[1][2].
References:
- [1]. Kennedy AJ, et al. International Union of Basic and Clinical Pharmacology CIII: Chemerin Receptors CMKLR1 (Chemerin1) and GPR1 (Chemerin2) Nomenclature, Pharmacology, and Function. Pharmacol Rev. 2018 Jan;70(1):174-196. [Content Brief]
- [2]. Zhang M, et al. G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery. Signal Transduct Target Ther. 2024 Apr 10;9(1):88. [Content Brief]
Chemerin Receptor Isoform Specific Products
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Chemerin Receptor Related Products (12)
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Chemerin Receptor Isoform Comparison
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α-NETA
0 Imagesα-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity. -
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Chemerin-9 (149-157) TFA
0 ImagesCat. No.: HY-P1844APurity: 98.41%Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism. -
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ChemR23-IN-1
0 ImagesChemR23-IN-1 (compound 2) is a ChemR23 inhibitor with IC50s of 38 nM and 100 nM for human and mouse ChemR23, respectively. ChemR23-IN-1 inhibits chemotaxis of CAL-1 triggered by Chemerin in vitro. -
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Resolvin E2
0 ImagesSynonyms: (-)-Resolvin E2Resolvin E2 ((-)-Resolvin E2) is an endogenous lipid mediator produced from eicosapentaenoic acid (EPA) under the catalysis of 5-lipoxygenase (5-LOX), and its production increases in hypoxic environments. Resolvin E2 antagonizes BLT1, partially activates ChemR23, and promotes ubiquitin-proteasome-mediated degradation of COX-2. Resolvin E2 reduces the production of prostaglandin E2, blocks polymorphonuclear leukocyte infiltration, and promotes the resolution of airway inflammation. Resolvin E2 ameliorates lipopolysaccharide (LPS) (HY-D1056)-induced depressive-like behaviors. Resolvin E2 can be used in research related to depression, murine peritonitis, neonatal asthma, and other conditions. -
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Chemerin15
0 ImagesChemerin15 is an anti-inflammatory peptide derived from Chemerin. Chemerin15 binds to ChemR23. Chemerin15 inhibits TNFα-induced activation of Syk, ERK and Src kinases. Chemerin15 increases the expression of p-p38 mRNA and protein. Chemerin15 mediates phagocytosis, resolution of inflammation, CD62L shedding and downregulation of PSGL-1 expression in macrophages and microglia. Chemerin15 inhibits neutrophil-mediated vascular inflammation and myocardial ischemia-reperfusion injury via ChemR23. Chemerin15 enhances microglial phagocytosis, thereby alleviating cerebral ischemia-reperfusion injury. -
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VU0514009
0 ImagesVU0514009 is a competitive chemokine-like receptor 1 (CMKLR1) antagonist (EC50=2 nM). VU0514009 prevents chemerin-9-induced arrestin recruitment and receptor internalization, significantly reducing Ca2+ flux response in HEK293 cells. VU0514009 is promising for research of inflammatory diseases and metabolic syndrome. -
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Urcosimod
0 ImagesCat. No.: HY-P11273CAS No.: 1610366-43-2Synonyms: OK 101Urcosimod (OK 101) is a lipid-coupled chemokine peptide, a ChemR23 G protein-coupled receptor agonist, which has been shown to have anti-inflammatory and analgesic activities. Urcosimod can be used for dry eye research. -
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Chemerin-9 (149-157)
0 ImagesChemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism. -
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ChemR23-IN-3
0 ImagesCat. No.: HY-145921CAS No.: 3032433-98-7ChemR23-IN-3 is a potent thiazole-based ChemR23 inhibitor with an IC80 value of 12 nM. -
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ChemR23-IN-4
0 ImagesCat. No.: HY-147642CAS No.: 2465085-23-6ChemR23-IN-4 (Compound 13) is a potent and orally efficacious ChemR23 inhibitor with an IC50 of 17 nM against human ChemR23. -
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Chemerin-9, mouse
0 ImagesCat. No.: HY-P2712CAS No.: 686324-96-9Synonyms: Chemerin148–156, mouseChemerin-9, mouse (Chemerin148-156, mouse) is a C-terminal nonapeptide of chemerin. Chemerin-9, mouse is a ligand for ChemR23 (EC50 = 42 nM). Chemerin-9, mouse reduces basal lipolysis in primary mouse white adipocytes(IC50 = 3.3 nM). Chemerin-9, mouse enhances memory and relieves Aβ1-42-induced memory impairment in AD mice. Chemerin-9, mouse also inhibits atherogenesis. -
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ChemR23-IN-2
0 ImagesCat. No.: HY-145352CAS No.: 2465086-50-2ChemR23-IN-2 is a potent and orally efficacious ChemR23 inhibitor with an IC50 value of 3.2 nM. -
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