235 Results for "

GPCR

" in MedChemExpress (MCE) Product Catalog:
Products (235)

235 Results for "GPCR" in MCE Product Catalog:

1
1 Cited Publications
Cat. No.: HY-157189
CAS No.: 898211-21-7
Purity:  99.72%
Synonyms: GPR132 antagonist 1
Target:  

G2A (GPR132)

Research Areas:  

Metabolic Disease

NOX-6-18 (GPR132 antagonist 1) is a GPR132 antagonist with an IC50 of 15.17 nM against the human target. NOX-6-18 inhibits GPR132 activation via interaction with non-conserved residues, blocks activities induced by endogenous agonists and 9 (S)-HODE, and exhibits selectivity for other fatty acid-binding GPCRs. NOX-6-18 regulates macrophage reprogramming, alleviates inflammatory responses, downregulates inflammatory markers and signaling pathways, and reduces the degree of hepatic steatosis and hepatic triglyceride levels. NOX-6-18 regulates metabolic homeostasis, reduces weight gain, enhances glucose metabolism, improves glucose tolerance, decreases fasting blood glucose and insulin levels, and partially reverses reductions in energy expenditure and respiratory quotient. NOX-6-18 can be used in the research of type 2 diabetes .
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Cat. No.: HY-107537
CAS No.: 264233-05-8
Purity:  99.35%
Target:  

GPR35

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM .
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Cat. No.: HY-N15721
CAS No.: 1630745-39-9
Synonyms: Trp-CA
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .
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Cat. No.: HY-141796
CAS No.: 2407452-77-9
Purity:  98.64%
Target:  

PROTACs WDR5

Research Areas:  

Cancer

MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
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Cat. No.: HY-103080
CAS No.: 1586787-08-7
Purity:  99.89%
Target:  

Apelin Receptor (APJ)

Research Areas:  

Cardiovascular Disease

CMF019 is an orally active, potent and small molecule agonist at Apelin receptor (APJ) with G protein bias. CMF019 binds to APJ with pKi values of 8.58, 8.49 and 8.71 for human, rat, and mouse, respectively. CMF019 mimics the beneficial cardiovascular actions of apelin in rodents . Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. CMF019 is promising for research of chronic diseases, such as, pulmonary arterial hypertension .
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Cat. No.: HY-P3137
CAS No.: 812644-79-4
Target:  

Angiotensin Receptor

Research Areas:  

Cardiovascular Disease

TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists .
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Cat. No.: HY-124803
CAS No.: 1407592-99-7
Target:  

GCGR

Research Areas:  

Metabolic Disease

GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes .
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Cat. No.: HY-177116
CAS No.: 252280-67-4
Target:  

HIV

Research Areas:  

Infection Inflammation/Immunology

GPR15 antagonist-1 (Compound 5) is a GPR15 antagonist. G protein-coupled receptor 15 (GPR15) is an extensively studied GPCRs involving HIV infection, colonic inflammation, and smoking-related diseases .
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Cat. No.: HY-P3136A
Synonyms: TRV120055 hydrochloride
Target:  

Angiotensin Receptor

Research Areas:  

Cardiovascular Disease

TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses [1]
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Cat. No.: HY-N0169R
CAS No.: 83-49-8
Synonyms: HDCA (Standard)
Hyodeoxycholic acid (Standard) is the analytical standard of Hyodeoxycholic acid. This product is intended for research and analytical applications. Hyodeoxycholic acid is a secondary bile acid formed in the small intestine by the gut flora, and acts as a TGR5 (GPCR19) agonist, with an EC50 of 31.6 µM in CHO cells.
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Cat. No.: HY-133862
CAS No.: 70375-43-8
SCH-202676 is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 µM .
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Cat. No.: HY-170589
CAS No.: 1574405-61-0
Research Areas:  

Neurological Disease

GPR17 antagonist 1 (compound 978) is a GPR17 antagonist. GPR17 antagonist 1 can be used in the study of diabetes and obesity .
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Cat. No.: HY-134801
CAS No.: 354126-20-8
Purity:  99.74%
Target:  

GPR35

CID1231538, a benzothiazole analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also a G protein-coupled receptor (GPCR) .
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Cat. No.: HY-110012
CAS No.: 265980-25-4
Purity:  96.81%
Target:  

Adenosine Receptor

Research Areas:  

Infection

SCH-202676 hydrobromide is an allosteric modulator of G protein-coupled receptors (GPCRs) and adenosine receptor (AR). SCH-202676 hydrobromide has antiviral activity and inhibits 3CL pro in a time-dependent manner with an IC50 value of 0.655 μM .
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Cat. No.: HY-119226
CAS No.: 612514-42-8
Purity:  98.25%
Target:  

mAChR

Research Areas:  

Neurological Disease

VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
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Cat. No.: HY-RS07620
Research Areas:  

Others

LGR6 Human Pre-designed siRNA Set A contains three designed siRNAs for LGR6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

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Cat. No.: HY-47823
CAS No.: 291528-35-3
Target:  

GPR109A

Research Areas:  

Metabolic Disease

GPCR agonist-2 (Compound 5j) is a GPCR GPR109b (HM74) agonist, with a pEC50 value of 6.51. GPCR agonist-2 can be used for research of lipid disorders .
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Cat. No.: HY-123737
CAS No.: 1431472-56-8
Research Areas:  

Neurological Disease

MK-8133 is an orexin-2 receptor antagonist. MK-8133 can be used in the study of insomnia .
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Cat. No.: HY-170973
Target:  

Opioid Receptor

KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
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Cat. No.: HY-12752
CAS No.: 84-96-8
Synonyms: Trimeprazine
Alimemazine is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.Alimemazine (Trimeprazine) is also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs. Alimemazine displays antiserotonin, antispasmodic, and antiemetic properties .
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