Scientific Reviews
Product Guides
Blogs
Topics
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
235 Results for "
GPCR
" in MedChemExpress (MCE) Product Catalog:
Products (235)
235 Results for "GPCR" in MCE Product Catalog:
Cat. No.: HY-14229R
CAS No.: 1197300-24-5
Synonyms: CCDC (Standard)
Research Areas:
TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity .
Cat. No.: HY-113918
Target:
Research Areas:
SW-106 is a selective antagonist of parathyroid hormone/parathyroid hormone-related peptide receptor (PPR) and PTHR1, with an IC50 value of 0.99 μM against PPR. SW-106 antagonizes cAMP responses. SW-106 can be used in the research of osteoporosis .
Cat. No.: HY-149168
CAS No.: 2292115-41-2
Target:
Research Areas:
PF-4211 is a selective non-catechol D1R agonist with a Ki value of 2.2 μM.. PF-4211 activates adenylate cyclase by binding to D1R, thereby increasing intracellular cAMP levels. PF-4211 can be used in research related to Parkinson's disease and schizophrenia .
Cat. No.: HY-D2930
Synonyms: SNAP-SS-SulfoCy5
Cat. No.: HY-115702S
CAS No.: 211106-54-6
Synonyms: (Rac)-PAF (C16)-d4
Research Areas:
2-Bromo-LSD (BOL-148) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD lacks 5-HT2B agonist activity. 2-Bromo-LSD induces dendritogenesis and spinogenesis. 2-Bromo-LSD reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
Cat. No.: HY-153830S
CAS No.: 2097249-92-6
Synonyms: C16 Lactosylceramide (d18:1/16:0)-d3
Cat. No.: HY-L150
7,133 compounds
Membrane receptors, also known cell surface receptors or transmembrane receptors, are transmembrane proteins embedded into the plasma membrane which play an essential role in maintaining communication between the internal processes within the cell and various types of extracellular signals. They act in cell signaling by receiving (binding to) extracellular molecules, which are also called ligands. These extracellular molecules include hormones, cytokines, growth factors, neurotransmitters, lipophilic signaling molecules such as prostaglandins, and cell recognition molecules.
There are three kinds of membrane receptors: ion channel-linked receptors, enzyme-linked receptors and G-protein-linked receptors. They play important roles in keeping human normal physiologic processes. GPCRs and ion channels are important drug targets in drug discovery.
MCE provides a unique collection of 7,133 compounds targeting a variety of membrane receptors. MCE Membrane reeptor-targeted Compound Library can be used for membrane receptor-focused screening and drug discovery.
Cat. No.: HY-L121
430 compounds
5-HT receptors, also called Serotonin receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. These receptors are now classified into seven families, 5-HT1–7, comprising a total of 14 structurally and pharmacologically distinct mammalian 5-HT receptor subtypes. The 5-HT receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.
MCE 5-HT Receptor Compound Library consists of 430 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.
Cat. No.: HY-184590
Target:
Research Areas:
AB12-82 is a selective dopamine receptor agonist with a Ki value of 1.88 nM for human D3R. AB12-82 achieves subtype-selective D3R activation by enhancing interactions with the D3R H291·32 residue. AB12-82 can be used in the research of nervous system-related diseases .
Cat. No.: HY-P702322
Purity: Purity analysis by SDS-PAGE is not available for VLP proteins.
Synonyms: HRH3; Histamine H3 Receptor Isoform 6; Histamine Receptor H3; Histamine H3 Receptor Isoform 5; GPCR97; Histamine H3 Receptor Isoform 3; Histamine H3 Receptor; G Protein-Coupled Receptor 97; HH3R; G-Protein Coupled Receptor 97; H3R
Species:
Human
Source:
HEK293
Cat. No.: HY-P702323
Purity: Purity analysis by SDS-PAGE is not available for VLP proteins.
Synonyms: HRH3; Histamine H3 Receptor Isoform 6; Histamine Receptor H3; Histamine H3 Receptor Isoform 5; GPCR97; Histamine H3 Receptor Isoform 3; Histamine H3 Receptor; G Protein-Coupled Receptor 97; HH3R; G-Protein Coupled Receptor 97; H3R
Species:
Human
Source:
HEK293
Cat. No.: HY-182697
CAS No.: 2130881-32-0
Target:
Research Areas:
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
Cat. No.: HY-184589
Target:
Research Areas:
AB13-46A is a selective dopamine receptor agonist, with a Ki value of 0.505 nM against human D3R. AB13-46A can be used for research on nervous system-related diseases .
Cat. No.: HY-157189A
Synonyms: GPR132 antagonist 1 (dihydrocholide)
Target:
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-L028
1,170 compounds
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 1,170 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
Cat. No.: HY-184591
Target:
Research Areas:
AB13-73A is a highly selective partial agonist of dopamine D3R, with a Ki of 0.803 nM and a pEC50 of 11.88 (1.32 pM). AB13-73A serves as a pharmacological tool to dissect the (patho) physiological mechanisms of D3R and support the development of improved neurotherapeutic agents .
Cat. No.: HY-N11798
CAS No.: 850894-19-8
Target:
Cat. No.: HY-P81150
Synonyms: G Protein Coupled Receptor 30; G-protein coupled receptor 30; G-protein coupled estrogen receptor 1; Membrane estrogen receptor; mER; Chemokine receptor-like 2; IL8-related receptor DRY12; Flow-induced endothelial G-protein coupled receptor 1; FEG-1; Lymphocyte-derived G-protein coupled receptor; LYGPR; GPCR-BR; CEPR; CMKRL2; DRY12; GPER.
Cat. No.: HY-121675A
CAS No.: 2855123-30-5
Synonyms: BOL-148 D-Tartrate; Bromolysergide D-Tartrate
Research Areas:
2-Bromo-LSD D-Tartrate (BOL-148 D-Tartrate) is a blood-brain barrier-permeable 5-HT2A partial agonist and competitive partial antagonist. 2-Bromo-LSD D-Tartrate acts as both a potent partial agonist (with an EC50 of 0.81 nM for Gq dissociation) and a potent partial antagonist (with a KB of 0.18 nM for Gq dissociation) at the 5-HT2A receptor. 2-Bromo-LSD D-Tartrate exhibits partial agonist activity at multiple aminergic GPCRs, including 5-HT2A. 2-Bromo-LSD D-Tartrate lacks 5-HT2B agonist activity. 2-Bromo-LSD D-Tartrate induces dendritogenesis and spinogenesis. 2-Bromo-LSD D-Tartrate reverses the behavioral effects of chronic stress and increases active coping behaviors in mice .
-
-
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
