- Signaling Pathways
- GPCR/G Protein
- Succinate Receptor 1
Succinate Receptor 1
SUCNR1; GPR91
The succinate receptor (SUCNR1, also known as GPR91) is a G protein-coupled receptor that is closely related to the family of P2Y purinoreceptors. The Succinate receptor was identified as being activated by physiological levels of the Kreb's cycle intermediate succinate and other dicarboxylic acids such as maleate. It is expressed in a variety of tissues, including blood cells, adipose tissue, the liver, retina, and kidney. In these tissues, this receptor and its ligand succinate have recently emerged as novel mediators in local stress situations, including ischemia, hypoxia, toxicity, and hyperglycemia. Amongst others, the succinate receptor is involved in recruitment of immune cells to transplanted tissues. Moreover, it was shown to play a key role in the development of diabetic retinopathy. However, most prominently, the role of locally increased succinate levels and succinate receptor activation in the kidney, stimulating the systemic and local renin–angiotensin system, starts to unfold: the succinate receptor is a key mediator in the development of hypertension and possibly fibrosis in diabetes mellitus and metabolic syndrome.
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Succinate Receptor 1 Related Products (10)
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NF-56-EJ40
0 ImagesNF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM. -
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cis-Epoxysuccinic acid
0 Imagescis-Epoxysuccinic acid is a succinate receptor (SUCNR1/GPR91) agonist. cis-Epoxysuccinic acid inhibits cAMP levels with an EC50 value of 2.7 μM. cis-Epoxysuccinic acid can be used for the research of cardiovascular system. -
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hGPR91 antagonist 1
0 ImageshGPR91 antagonist 1 (Compound 4c) is a potent and selective GPR91 antagonist with an IC50 of 7 nM for human GPR91. -
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Succinate/succinate receptor antagonist 1
0 ImagesSuccinate/succinate receptor antagonist 1 is an antagonist of the succinate/succinate receptor. Succinate/succinate receptor antagonist 1 can inhibit the activation of succinate receptor 1 (SUCNR1). Succinate/succinate receptor antagonist 1 can block succinate signaling. Succinate/succinate receptor antagonist 1 can be used for the study of periodontal disease. -
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SUCNR1-IN-1
0 ImagesSUCNR1-IN-1 is an orally active SUCNR1 inhibitor. SUCNR1-IN-1 exhibits inhibitory rates of 23% and 56% against rat and mouse SUCNR1 at 100 μM, respectively. SUCNR1-IN-1 can be used in the research of rheumatoid arthritis. -
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SUCNR1 antagonist-1
0 ImagesCat. No.: HY-183639SUCNR1 antagonist-1 is an orally active SUCNR1 antagonist. SUCNR1 antagonist-1 forms stable, water-bridged hydrogen bonds with key residue Glu221.31 to stabilize binding conformation and modulates protein conformational flexibility. SUCNR1 antagonist-1 blocks succinate-mediated SUCNR1 signaling and induces cell apoptosis. SUCNR1 antagonist-1 can be used for the research of colorectal carcinoma. -
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hGPR91 antagonist 3
0 ImageshGPR91 antagonist 3 (Compound 5g) is a potent and orally active GPR91 antagonist with IC50s of 35 nM and 135 nM, for human GPR91 and rat GPR91, respectively. -
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SUCNR1-IN-2
0 ImagesSUCNR1-IN-2 (Statement 35) is a SUCNR1 inhibitor. SUCNR1-IN-2 can be used for the study of neurodegenerative diseases such as neuroinflammation. -
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NF-56-EJ40 hydrochloride
0 ImagesNF-56-EJ40 hydrochloride is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 hydrochloride has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM. -
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4'-O-Methylbavachalcone
0 Images4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy. -
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