Search Result

Pathways Recommended:	GPCR/G Protein

Results for "

G-protein coupled receptors (GPCRs)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	G protein-coupled Bile Acid Receptor 1 (2) G Protein-coupled Receptor Kinase (GRK) (1) GPR35 (1) GPR68 (1) Adenosine Receptor (2) Angiotensin Receptor (3) Apelin Receptor (APJ) (1) Apoptosis (4) Calcium Channel (1) CCR (1) Free Fatty Acid Receptor (1) Influenza Virus (1) Isotope-Labeled Compounds (2) Melatonin Receptor (1) Opioid Receptor (1) Potassium Channel (1) Trace Amine-associated Receptor (TAAR) (2) Vasopressin Receptor (1)
By Research Areas:	Cancer (6) Cardiovascular Disease (8) Endocrinology (3) Infection (3) Inflammation/Immunology (3) Metabolic Disease (5) Neurological Disease (7)

By Targets:

G protein-coupled Bile Acid Receptor 1 (2)

G Protein-coupled Receptor Kinase (GRK) (1)

GPR35 (1)

GPR68 (1)

Adenosine Receptor (2)

Angiotensin Receptor (3)

Apelin Receptor (APJ) (1)

Apoptosis (4)

Calcium Channel (1)

CCR (1)

Free Fatty Acid Receptor (1)

Influenza Virus (1)

Isotope-Labeled Compounds (2)

Melatonin Receptor (1)

Opioid Receptor (1)

Potassium Channel (1)

Trace Amine-associated Receptor (TAAR) (2)

Vasopressin Receptor (1)

By Research Areas:

Cancer (6)

Cardiovascular Disease (8)

Endocrinology (3)

Infection (3)

Inflammation/Immunology (3)

Metabolic Disease (5)

Neurological Disease (7)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: G Protein-coupled Receptor Kinase (GRK) Mas-related G-protein-coupled Receptor (MRGPR) GPR84 G protein-coupled Bile Acid Receptor 1 GPR55 GPR88 GPR171 GPR35 GPR119 GPR4 GPR139 GPR6 GPR52 GPR68

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-134801

CID1231538	GPR35	Metabolic Disease Inflammation/Immunology
CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC₅₀=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR) .

HY-129118

Takeda103A	Others	Cardiovascular Disease
Takeda103A is a potent inhibitor of GRK2. G protein-coupled receptors (GPCRs) are central to many physiological processes. Takeda103A has the potential for the research of heart failure .

HY-148531

PF-07054894	CCR	Inflammation/Immunology
PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease .

HY-103080

CMF019	Apelin Receptor (APJ)	Cardiovascular Disease
CMF019 is a 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 .

HY-P0049A

Argipressin diacetate Arg8-vasopressin diacetate; AVP diacetate; ADH	Apoptosis Vasopressin Receptor	Neurological Disease
Argipressin (diacetate) (AVP (diacetate), also known as antidiuretic hormone (ADH)) is a 9 amino acid neuropeptide secreted by the posterior pituitary. Argipressin (diacetate) (AVP (diacetate)) can regulate the biological effects of fluid balance, osmolality and cardiovascular through three separate G-protein coupled receptors (GPCRs), namely Avpr1a (V1a), Avpr1b (V1b) and Avpr2 (V2). Argipressin (diacetate) (AVP (diacetate)) also have potentially important effects on centrally regulated metabolic processes .

HY-133862

SCH-202676	Influenza Virus G protein-coupled Bile Acid Receptor 1 Adenosine Receptor	Infection
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 .

HY-147542

Melatonin receptor agonist 1	Melatonin Receptor	Neurological Disease
Melatonin receptor agonist 1 (compound 20c) is a potent melatonin receptor (MT) agonist, with K_i values of 108 nM (MT₂) and 1140 nM (MT₁) .

HY-110012

SCH-202676 hydrobromide	Adenosine Receptor	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 .

HY-101483

Dihydromunduletone DHM	Others	Neurological Disease Cancer
Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent *adhesion G protein-coupled* receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC ₅₀ of 20.9 μM for GPR56*, but not inhibit GPR110 or class A GPCRs* .

HY-110098

Ro 5212773 EPPTB	Trace Amine-associated Receptor (TAAR)	Neurological Disease
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (K_i=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids .

HY-134494

MS48107	GPR68	Neurological Disease
MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .

HY-47573

CCG273441	G Protein-coupled Receptor Kinase (GRK)	Cardiovascular Disease Cancer
CCG273441 is a covalent inhibitor of G protein-coupled receptor (GPCR) kinase 5 (GRK5) with an IC₅₀ value of 3.8 nM. CCG273441 is highly selective to GRK5 over GRK2 (IC₅₀=4.8 μM) by binding Cys474, a GRK5 subfamily-specific residue, as a covalent handle .

HY-113478S

Ursodeoxycholic acid-2,2,4,4-d4	Isotope-Labeled Compounds	Infection Metabolic Disease
Ursodeoxycholic acid-2,2,4,4-d₄ is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection[1][2][3][4][5].

HY-139690

CCG258747	Opioid Receptor	Cardiovascular Disease
CCG258747 is a selective GRK2 inhibitor (IC₅₀=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure .

HY-160281

CCD-2	Others	Metabolic Disease
CCD-2 is a conventional detergent and is readily degraded. CCD-2 can efficiently solubilize and stabilize diverse G protein-coupled receptors (GPCRs). CCD-2 is amenable to the β-barrel protein research. The chemical cleavage of CCD-2 is rapid, complete and biorthogonal and should facilitate a chemical methodology for in situ detergent replacement in diverse membrane proteins (MPs) studies .

HY-12700

RO5256390 1 Publications Verification	Trace Amine-associated Receptor (TAAR)	Neurological Disease
RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of agents of abuse through their actions on the mesocorticolimbic system . RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic agent olanzapine, suggesting antipsychotic-like properties .

HY-15589

GW9508 4 Publications Verification	Free Fatty Acid Receptor Potassium Channel	Cardiovascular Disease Metabolic Disease Inflammation/Immunology
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 (K_ATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities .

HY-14229

TGR5 Receptor Agonist 1 Publications Verification CCDC	G protein-coupled Bile Acid Receptor 1 Calcium Channel	Metabolic Disease
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 Ca ²⁺ 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 .

HY-13948BS

Angiotensin II human-13C6,15N TFA Angiotensin II-13C₆,¹⁵N TFA; Ang II-13C₆,¹⁵N TFA; DRVY(I-13C₆,¹⁵N)HPF TFA	Isotope-Labeled Compounds	Cancer
Angiotensin II human- ¹³C₆, ¹⁵N TFA (Ang II- ¹³C₆, ¹⁵N TFA) is ¹³C- and ¹⁵N-labeled Angiotensin II human (TFA) (HY-13948B). Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions .

HY-13948

Angiotensin II human Maximum Cited Publications 93 Publications Verification Angiotensin II; Ang II; DRVYIHPF	Angiotensin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Angiotensin II (Angiotensin II) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .

HY-13948A

Angiotensin II human acetate Maximum Cited Publications 93 Publications Verification Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate	Angiotensin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .

HY-13948B

Angiotensin II human TFA Maximum Cited Publications 93 Publications Verification Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA	Angiotensin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library	2286 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 2286 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

GPCR/G Protein Compound Library

2286 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 2286 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

HY-L121

5-HT Receptor Compound Library	307 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 307 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

5-HT Receptor Compound Library

307 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 307 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

HY-L013

Neuronal Signaling Compound Library	2542 compounds
Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders. MCE designs a unique collection of 2542 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Neuronal Signaling Compound Library

2542 compounds

Neuronal Signaling is involved in the regulation of the mechanisms of the central nervous system (CNS) such as its structure, function, genetics and physiology as well as how this can be applied to understand diseases of the nervous system. Every information processing system in the CNS is composed of neurons and glia, neurons have evolved unique capabilities for intracellular signaling (communication within the cell) and intercellular signaling (communication between cells). G protein-coupled receptors (GPCRs), including 5-HT receptor, histamine receptor, opioid receptor, etc. are the largest class of sensory proteins and are important therapeutic targets in Neuronal Signaling. Besides, Notch signaling, such as β- and γ-secretase, also plays multiple roles in the development of the CNS including regulating neural stem cell (NSC) proliferation, survival, self-renewal and differentiation. GPCR dysfunction caused by receptor mutations and environmental challenges contributes to many neurological diseases. Notch signaling in neurons, glia, and NSCs is also involved in pathological changes that occur in disorders such as stroke, Alzheimer's disease and CNS tumors. Thus, targeting Neuronal Signaling, such as notch signaling and GPCRs, can be used as therapeutic interventions for several different CNS disorders.

MCE designs a unique collection of 2542 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Cat. No.	Product Name	Target	Research Area