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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
235 Results for "
GPCR
" in MedChemExpress (MCE) Product Catalog:
Products (235)
235 Results for "GPCR" in MCE Product Catalog:
Cat. No.: HY-145156
CAS No.: 2212020-93-2
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CHU-128 is an effective and selective GLP-1R agonist. CHU-128 exhibits strong signal specificity and can activate the Gs/cAMP pathway, but it cannot activate the Gq/calcium signal, ERK phosphorylation, or recruit β-inhibitory proteins. CHU-128 can be used for research on type 2 diabetes .
Cat. No.: HY-147908
CAS No.: 2550401-76-6
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Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR .
Cat. No.: HY-129636
CAS No.: 1611483-29-4
Synonyms: (E)-GABAB receptor antagonist 1
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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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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)
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ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research .
Cat. No.: HY-P1130
CAS No.: 908844-75-7
Synonyms: Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide
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Cat. No.: HY-10499R
CAS No.: 892546-37-1
Synonyms: BIM-46187 (Standard)
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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 .
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Cat. No.: HY-180583
CAS No.: 3061801-11-1
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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)
Cat. No.: HY-L158
6,342 compounds
According to reports, most known kinase inhibitors exert their effects through competitive binding in highly conserved ATP pockets. Although genetic techniques such as RNA interference can inactivate specific genes, most kinases are multi domain proteins, each of which has an independent function. Highly selective inhibitors have higher efficiency than non-selective inhibitors, and the selectivity to the target is at least 100 times higher. Therefore, ensuring the validation of targets with the most selective inhibitors is crucial for a more thorough understanding of the pharmacology of the kinase field. The Highly Selective Inhibitors Library contains 6,342 compounds, covering multiple targets and subtypes, such as GPCR protein family, Ion channel, multiple kinases, etc. The Highly Selective Inhibitors Library is an effective tool for screening different phenotypes
Cat. No.: HY-10805AR
CAS No.: 913358-93-7
Synonyms: ACT 078573 hydrochloride (Standard)
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Almorexant hydrochloride (Standard) is the analytical standard of Almorexant (hydrochloride) (HY-10805A). This product is intended for research and analytical applications. Almorexant (ACT 078573) hydrochloride is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
Cat. No.: HY-10805R
CAS No.: 871224-64-5
Synonyms: ACT 078573 (Standard)
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Almorexant (Standard) is the analytical standard of Almorexant. This product is intended for research and analytical applications. Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis .
Cat. No.: HY-P87577
Synonyms: GPR80, GPR99, P2RY15, P2Y15, OXGR1, 2-oxoglutarate receptor 1, Alpha-ketoglutarate receptor 1, G-protein coupled receptor 80, G-protein coupled receptor 99, P2Y purinoceptor 15, P2Y-like GPCR, P2Y-like nucleotide receptor
Cat. No.: HY-13948BS
Purity: 98.11%
Synonyms: Angiotensin II-13C6,15N TFA; Ang II-13C6,15N TFA; DRVY(I-13C6,15N)HPF TFA
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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
