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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
164 Results for "
GPCR multimer
" in MedChemExpress (MCE) Product Catalog:
Products (164)
164 Results for "GPCR multimer" in MCE Product Catalog:
Cat. No.: HY-10499A
CAS No.: 2489449-03-6
Synonyms: BIM-46187 tetrahydrochloride
Target:
Research Areas:
PH-064 tetrahydrochloride (BIM-46187 tetrahydrochloride) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 tetrahydrochloride inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 tetrahydrochloride has potent anti-hyperalgesia activity. PH-064 tetrahydrochloride inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 tetrahydrochloride can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury .
Cat. No.: HY-115702
CAS No.: 77286-68-1
Synonyms: (Rac)-PAF (C16)
Research Areas:
1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine ((Rac)-PAF (C16)) is an endogenous inflammatory lipid mediator. 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine acts as a high-affinity agonist for PAFR (GPCR), inducing platelet aggregation, vascular permeability, and leukocyte chemotaxis at extremely low concentrations. 1-Palmityl-2-O-acetyl-3-glyceryl phosphorylcholine exerts its effects via cell surface receptors to regulate inflammation .
Cat. No.: HY-122351
CAS No.: 245650-17-3
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Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
Target:
Research Areas:
Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
Cat. No.: HY-181287
Target:
Research Areas:
PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease .
Cat. No.: HY-W010516
CAS No.: 97-61-0
Synonyms: 2-Methylpentanoic acid
Category:
Ketones, Aldehydes, Acids Metabolic Disease Plants Other Families Extract Endogenous metabolite Disease Research Fields
Target:
Cat. No.: HY-W339834
CAS No.: 325465-92-7
Research Areas:
1-Stearoyl-sn-glycerol 3-phosphate sodium is a bioactive phospholipid that plays a crucial role in modulating cellular processes such as motility, proliferation, invasion, survival, and growth factor production, primarily through its interaction with G protein-coupled receptors (GPCRs). Typically found at low concentrations in plasma (~100nM), this compound is synthesized during the formation of membrane phospholipids and is derived from various cell types, including activated platelets, epithelial cells, leukocytes, neuronal cells, and tumor cells. Its unique structure includes stearic acid at the sn-1 position alongside a hydroxyl group at the sn-2 position.
Cat. No.: HY-L159
2,192 compounds
Agonistic drugs activate or stimulate their receptors, triggering responses that increase or decrease cell activity. The highly selective activators can act on specific biological or molecular targets, while non-selective activators may interfere with multiple targets or targets simultaneously. The highly selective activators reduce the likelihood of these non-specific effects by targeting specific targets, making research more precise and reliable. The Highly Selective Activators Library contains 2,192 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Activators Library is an effective tool for screening different phenotypes.
Cat. No.: HY-103080R
CAS No.: 1586787-08-7
Research Areas:
CMF019 (Standard) is the analytical standard of CMF019 (HY-103080). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-129636
CAS No.: 1611483-29-4
Synonyms: (E)-GABAB receptor antagonist 1
Target:
Research Areas:
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
Cat. No.: HY-15589R
CAS No.: 885101-89-3
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
GW9508 (Standard) is the analytical standard of GW9508. This product is intended for research and analytical applications. GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .
Cat. No.: HY-184442
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Research Areas:
GPR132 antagonist-2 is a G2A (GPR132) antagonist with an IC50 of 0.69 μM. GPR132 antagonist-2 exerts weak stabilizing effects on the bromodomain of BRD2 and exhibits selectivity for non-olfactory GPCRs. GPR132 antagonist-2 inhibits G2A activation, blocks downstream inositol monophosphate accumulation, reverses G2A-mediated TRPV1 sensitization, suppresses 9-HODE-mediated capsaicin-induced TRPV1 responses, and activates FPR3. GPR132 antagonist-2 can be used in studies related to neuropathic pain .
Cat. No.: HY-W010448R
CAS No.: 22884-10-2
Cat. No.: HY-L949
1279 compounds
Spirocyclic compounds, with rigid 3D structures, high Fsp³ and strong conformational restriction, are highly privileged scaffolds in small-molecule drug screening. They overcome drawbacks of planar aromatic compounds such as poor solubility, high off-target risks and weak druggability. Their orthogonal bicyclic geometry fits well into protein pockets, improving target affinity, subtype selectivity, metabolic stability and membrane permeability, making them ideal for hit identification against kinases, GPCRs, PPIs and other targets.
Spirocyclic scaffolds have been widely applied in oncology, antivirals, hypertension and CNS diseases, leading to many approved drugs and clinical candidates. SAR studies show that spiro-atom chirality, ring size and heteroatom substitution dominate bioactivity and selectivity, with the scaffold mainly serving as a conformational anchor. Azaspirocycles, spirooxindoles and spirosteranes target GPCRs, kinases, MDM2-p53 and PPIs. Approved drugs including irbesartan, spironolactone and rolapitant confirm their druggability, while revumenib and SAR405838 show promise against undruggable targets.
The MCE Spirocyclic Druglike Library contains over 1,000 diverse, stereospecific molecules selected by Lipinski’s rules. It covers privileged cores such as azaspirocycles, oxaspirocycles and spirooxindoles. These molecules bear rich chiral centers and distinct 3D orientations, reducing non-specific binding and enhancing screening efficiency. Featuring novel scaffolds, the library offers a highly innovative starting point for drug discovery.
Cat. No.: HY-122351AR
CAS No.: 714229-20-6
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Advantame (Standard) is the analytical standard of Advantame. This product is intended for research and analytical applications. Advantame is an N-substituted derivative of aspartame. Advantame is a high-intensity, low calorie sweetener. Advantame can interact with plasma protein. Advantame has the potential to produce hypotension and inhibit hERG K + channel to produce carditoxicity. Advantame binds to T1R2/T1R3 taste GPCR to form an oligomeric functional selectivity of biased heteromers with NMBR to induce a significant sialidase activity in vitro. Advantame has maternal toxicity (gastrointestinal disturbances) in the prenatal developmental toxicity study in rabbits .
Synonyms: Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)
Cat. No.: HY-10499R
CAS No.: 892546-37-1
Synonyms: BIM-46187 (Standard)
Research Areas:
PH-064 (Standard) is the analytical standard of PH-064 (HY-10499). This product is intended for research and analytical applications. PH-064 (BIM-46187) is an orally active inhibitor of the heterotrimeric G-protein complex. PH-064 inhibits SERT activity and attenuates shear stress-induced Akt phosphorylation. PH-064 has potent anti-hyperalgesia activity. PH-064 inhibits G protein-coupled receptor-dependent tumorigenesis. PH-064 can be used in the study of pain (e.g., inflammatory pain, neuropathic pain), GPCR-dependent tumors, and inflammatory lung injury .
Category:
Target:
Cat. No.: HY-180583
CAS No.: 3061801-11-1
Research Areas:
GRK5-IN-5 (Compound 4a) is a selective G protein-coupled receptor (GPCR) kinase 5 (GRK5) inhibitor with an IC50 of 0.03 μM. GRK5-IN-5 shows IC50 values of 2.2 and 0.036 μM for GRK2 and GRK6. GRK5-IN-5 has potent anti-myocardial hypertrophy activity and also inhibits the proliferation of non-myocardial cells. GRK5-IN-5 can inhibit the abnormal upregulation of hypertrophy marker genes Nppa and Nppb, thus blocking pathological myocardial remodeling. GRK5-IN-5 can be used for the research of cardiac hypertrophy .
Cat. No.: HY-W010516R
CAS No.: 97-61-0
Synonyms: 2-Methylpentanoic acid (Standard)
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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
