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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
GPCR signaling
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "GPCR signaling" in MCE Product Catalog:
32
32 Publications Verification
Synonyms: Ursodeoxycholate; Ursodiol; UDCA
32
32 Publications Verification
Synonyms: Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium
2
2 Cited Publications
Target:
Research Areas:
ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons .
1
1 Cited Publications
Synonyms: Ursodeoxycholate-d4; Ursodiol-d4; UDCA-d4
1
1 Cited Publications
Synonyms: GPR132 antagonist 1
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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 .
1
Synonyms: Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)
Cat. No.: HY-P4776
CAS No.: 202463-00-1
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Cat. No.: HY-P10365
Research Areas:
Cat. No.: HY-13771S1
CAS No.: 63296-46-8
Synonyms: Ursodeoxycholate-13C; Ursodiol-13C; UDCA-13C
Cat. No.: HY-W783254
CAS No.: 799279-67-7
Synonyms: PA(18:0e/0:0)
Research Areas:
C18 LPA (PA(18:0e/0:0)) is a water-soluble phospholipid that functions as a signaling molecule, influencing various cellular responses through G protein-coupled receptors (GPCRs). It is known to promote smooth muscle contraction, cytoskeletal rearrangement, and chemotaxis, while also playing a role in neurotransmitter release, cell proliferation, platelet aggregation, and Ca2+ mobilization. Elevated levels of C18 LPA in human plasma are associated with ovarian cancer and atherosclerosis, suggesting its potential as a biomarker for ovarian cancer.
Cat. No.: HY-168997
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CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating Gi/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain .
Cat. No.: HY-179240
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UNC9815 is a D1 dopamine receptor (D1R) orthosteric allosteric modulator (PAM). UNC9815 can dose-dependently enhance the functional efficacy of dopamine in β-inhibitory protein recruitment experiments and cAMP accumulation experiments. When used in combination with other PAMs, UNC9815 exhibits a significant synergistic enhancement effect. UNC9815 can be used to study neurological and psychiatric diseases such as Parkinson's disease and schizophrenia .
Cat. No.: HY-D2984
CAS No.: 1308789-62-9
Synonyms: SNAP-PEG-NH2
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BG-PEG-NH2 (SNAP-PEG-NH2) is an amino-terminal fluorescent probe building block and a precursor for site-specific labeling of SNAP-tag fusion proteins. BG-PEG-NH2 undergoes one-step coupling with activated carboxyl esters to form customized SNAP-tag substrates, which covalently bind to SNAP tags via a thioether bond formed at the Cys145 site. After coupling with a caged carboxyfluorescein, BG-PEG-NH2 forms a probe with Ex/Em = 500/524 nm following ultraviolet uncaging. Coupling of BG-PEG-NH2 with SeTau-647-NHS enables visualization of GPCR signal transduction. BG-PEG-NH2 is suitable for coupling reactions in aqueous phases or buffers, conjugation of labels, and labeling of intracellular or cell-surface proteins .
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CCG-4986 is an RGS protein inhibitor. CCG-4986 inhibits protein activity by covalently modifying the Cys-132 site of RGS4. CCG-4986 can be used to study diseases related to dysregulated G protein-coupled receptor (GPCR) signaling, such as Parkinson's disease and opioid addiction .
Cat. No.: HY-126748
CAS No.: 2223023-78-5
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VUF14862 is a stable and fatigue-resistant photoswitchable GPCR antagonist targeting the histamine H3 receptor (H3R) pathway. VUF14862 binds to H3R with >10-fold increased affinity upon 360 nm irradiation. VUF14862 can be used for spatiotemporal studies of H3R signaling .
Cat. No.: HY-157189A
Synonyms: GPR132 antagonist 1 (dihydrocholide)
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Research Areas:
NOX-6-18 (dihydrocholide) (GPR132 antagonist 1 (diHYdrocholide)) is a GPR132 antagonist with an IC50 of 15.17 nM against the human target. NOX-6-18 (dihydrocholide) 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 (dihydrocholide) 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 (dihydrocholide) 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 (dihydrocholide) can be used in the research of type 2 diabetes .
Cat. No.: HY-L006
3,519 compounds
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.
MCE provides a unique collection of 3,519 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.
Cat. No.: HY-183400
CAS No.: 195450-11-4
Target:
Neurotensin Receptor MMP EGFR Toll-like Receptor (TLR) Wnt Caspase PARP MyD88 NF-κB TNF Receptor Apoptosis
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BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia .
Cat. No.: HY-187642
CAS No.: 303059-39-4
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IGGi-11 is a competitive Gαi inhibitor with a Kd of 5.3 μM for sGαi3. IGGi-11 binds to the GIV interaction region of Gαi3, blocks non-canonical G protein signaling, and does not interfere with Gαi nucleotide processing, Gβγ binding, GPCR activation, or effector regulation. IGGi-11 inhibits the pro-invasive properties of metastatic breast cancer. IGGi-11 can be used in related studies on metastatic breast cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
