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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 (5) G Protein-coupled Receptor Kinase (GRK) (1) GPR35 (1) GPR68 (1) Adenosine Receptor (2) Angiotensin Receptor (3) Angiotensin-converting Enzyme (ACE) (1) Apelin Receptor (APJ) (1) Apoptosis (4) Calcium Channel (1) CCR (1) Endogenous Metabolite (4) Free Fatty Acid Receptor (1) FXR (3) Influenza Virus (1) Isotope-Labeled Compounds (3) Neuropeptide B/W Receptor (2) Opioid Receptor (1) Potassium Channel (2) RGS Protein (1) Trace Amine-associated Receptor (TAAR) (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (12) Cardiovascular Disease (9) Endocrinology (3) Infection (4) Inflammation/Immunology (5) Metabolic Disease (7) Neurological Disease (9)
Oligonucleotides:	Nucleotides and their Analogs (1) Phospholipids (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

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 analog, is a potent GPR35 antagonist with no significant activity against rodent orthologs of GPR35, which is also 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-101483

Dihydromunduletone 1 Publications Verification	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-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-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-W019895

Tetradecylphosphocholine	Others	Others
Tetradecylphosphocholine is a zwitterionic surfactant that can be used as a detergent for membrane protein solubilization .

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-122251

CCG-4986	RGS Protein	Others Neurological Disease
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 .

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-148531

PF-07054894	CCR	Inflammation/Immunology
PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC₅₀ value of 5.7 nM in vitro. 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 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 .

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-15589

GW9508 5 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 2 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-W339834

1-Stearoyl-sn-glycerol 3-phosphate sodium	Others	Others
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.

HY-13771A

Ursodeoxycholic acid sodium 10+ Cited Publications Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium	G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite	Metabolic Disease Inflammation/Immunology Cancer
Ursodeoxycholic acid (Ursodeoxycholate) sodium 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 sodium 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 sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .

HY-P10289

Neuropeptide W-30 (rat) NPW30, rat	Neuropeptide B/W Receptor	Neurological Disease
Neuropeptide W-30 (rat) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (rat) is an endogenous ligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. NPW-30 activates and binds to both GPR7 and GPR8 at similar effective doses .

HY-13771S1

Ursodeoxycholic acid-13C Ursodeoxycholate-¹³C; Ursodiol-¹³C; UDCA-¹³C	Isotope-Labeled Compounds G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite	Cancer
Ursodeoxycholic acid- ¹³C is the ¹³C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) 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. Orally active[1][2].

HY-P0049A

Argipressin diacetate Arg8-vasopressin diacetate; AVP diacetate; ADH	Apoptosis Vasopressin Receptor	Neurological Disease Cancer
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-P10287

Neuropeptide W-30 (human) NPW30, human	Neuropeptide B/W Receptor	Neurological Disease
Neuropeptide W-30 (human) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (human) is an endogenous ligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. Neuropeptide W-30 (human) activates and binds to both GPR7 and GPR8 at similar effective doses .

HY-13771

Ursodeoxycholic acid 10+ Cited Publications Ursodeoxycholate; Ursodiol; UDCA	G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite	Infection Metabolic Disease Cancer
Ursodeoxycholic acid (Ursodeoxycholate) 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. Orally active .

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-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 112 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 112 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 112 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 .

HY-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt	Endogenous Metabolite Potassium Channel	Neurological Disease Inflammation/Immunology Cancer
Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K ⁺ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library	2,437 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 2,437 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

2,437 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 2,437 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	317 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 317 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

5-HT Receptor Compound Library

317 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 317 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

HY-L013

Neuronal Signaling Compound Library	2,733 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 2,733 Neuronal Signaling-related compounds that act as a useful tool for the research of neuronal regulation and neuronal diseases.

Neuronal Signaling Compound Library

2,733 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 2,733 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

HY-P10365

VPM-p15	Peptides	Others
Vmm-p15 is a peptide agonist optimized for the adhesion G protein-coupled receptor GPR64 (also known as ADGRG2 or HE6). The affinity of VPM-p15 with GPR64 is significantly higher than that of the original p15 peptide. The cAMP level induced by VMM-P15 increased significantly, activated GPR64, and triggered downstream Gs, Gq, and G12/13 signaling. VPM-p15 can be used to study the activation mechanism of adherent GPCR family members .

HY-13948

Angiotensin II human Maximum Cited Publications 112 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 112 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 112 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 .

HY-P5084

Neuromedin S (human)	Peptides	Neurological Disease
Neuromedin S (human) is a neuropeptide that contains 33 amino acids.? Neuromedin S (human)has been identified in the brain as an endogenous ligand for the orphan *G-protein coupled* receptor (GPCR) FM-4/TGR-1 and acts on the neuromedin U (NMU) receptor 2 (NMUR2)** in the regulation of body weight homeostasis .

HY-P10289

Neuropeptide W-30 (rat) NPW30, rat	Neuropeptide B/W Receptor	Neurological Disease
Neuropeptide W-30 (rat) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (rat) is an endogenous ligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. NPW-30 activates and binds to both GPR7 and GPR8 at similar effective doses .

HY-P0049A

Argipressin diacetate Arg8-vasopressin diacetate; AVP diacetate; ADH	Apoptosis Vasopressin Receptor	Neurological Disease Cancer
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-P10287

Neuropeptide W-30 (human) NPW30, human	Neuropeptide B/W Receptor	Neurological Disease
Neuropeptide W-30 (human) is an important stress mediator in the central nervous system that modulates the hypothalamus-pituitary-adrenal (HPA) axis and sympathetic outflow. Neuropeptide W-30 (human) is an endogenous ligand for the two structurally related orphan G-protein-coupled receptors (GPCRs) GPR7 and GPR8. Neuropeptide W-30 (human) activates and binds to both GPR7 and GPR8 at similar effective doses .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13771A

Ursodeoxycholic acid sodium 10+ Cited Publications Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium	Structural Classification Microorganisms Classification of Application Fields Source classification Metabolic Disease Inflammation/Immunology Disease Research Fields Steroids	G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite
Ursodeoxycholic acid (Ursodeoxycholate) sodium 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 sodium 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 sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .

HY-13771

Ursodeoxycholic acid 10+ Cited Publications Ursodeoxycholate; Ursodiol; UDCA	Structural Classification Human Gut Microbiota Metabolites Microorganisms Other disease Classification of Application Fields Source classification Disease markers Endogenous metabolite Disease Research Fields Steroids Cancer	G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite
Ursodeoxycholic acid (Ursodeoxycholate) 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. Orally active .

HY-13948

Angiotensin II human Maximum Cited Publications 112 Publications Verification Angiotensin II; Ang II; DRVYIHPF	Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields Endocrinology Cancer	Angiotensin Receptor Apoptosis
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-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt	Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	Endogenous Metabolite Potassium Channel
Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K ⁺ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .

Cat. No.	Product Name	Chemical Structure

HY-113478S

Ursodeoxycholic acid-2,2,4,4-d4

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-13948BS

Angiotensin II human-13C6,15N TFA

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-13771S1

Ursodeoxycholic acid-13C

Ursodeoxycholic acid- ¹³C is the ¹³C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) 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. Orally active[1][2].

Cat. No.	Product Name		Classification

HY-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt		Nucleotides and their Analogs
Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K ⁺ channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .

HY-W783254

C18 LPA PA(18:0e/0:0)		Phospholipids
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.

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