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Pathways Recommended:	GPCR/G Protein

Results for "

G protein-coupled receptor (GPCR)

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Adhesion G Protein-coupled Receptors (AGPCRs) (1) G protein-coupled Bile Acid Receptor 1 (8) G Protein-coupled Receptor Kinase (GRK) (4) GPR35 (1) GPR68 (1) Orphan GPCR (1) 5-HT Receptor (1) Acyltransferase (1) Adenosine Receptor (3) Akt (3) Angiotensin Receptor (3) Angiotensin-converting Enzyme (ACE) (2) Apelin Receptor (APJ) (2) Apoptosis (4) Aryl Hydrocarbon Receptor (1) Calcium Channel (3) CCR (2) Drug Derivative (3) Endogenous Metabolite (12) ERK (1) Free Fatty Acid Receptor (3) FXR (4) GCGR (3) GLP Receptor (3) Hepcidin (2) HIV (1) Influenza Virus (1) Isotope-Labeled Compounds (4) Liposome (1) Neuromedin U Receptor (NMUR) (1) Neuropeptide B/W Receptor (3) Neuropeptide Y Receptor (2) Parasite (1) Phosphatase (1) PI3K (1) Potassium Channel (4) Ras (1) Reference Standards (8) RGS Protein (1) Serotonin Transporter (3) Trace Amine-associated Receptor (TAAR) (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (11) Infection (9) Inflammation/Immunology (16) Metabolic Disease (22) Neurological Disease (19)
Oligonucleotides:	Nucleotide Analogs (1) Phospholipids (1)

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Screening Libraries

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Inhibitory Antibodies

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Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Oligonucleotides

Targets Recommended: Orphan GPCR G protein-coupled Bile Acid Receptor 1 GPR55 GPR88 GPR171 GPR35 GPR119 G Protein-coupled Receptor Kinase (GRK) GPR4 GPR139 GPR6 GPR65 GPR52 GPR68 Adhesion G Protein-coupled Receptors (AGPCRs)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13948

Angiotensin II human Maximum Cited Publications 222 Publications Verification Angiotensin II; Ang II; DRVYIHPF	Angiotensin Receptor Apoptosis	Cardiovascular Disease Infection Metabolic Disease Inflammation/Immunology 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-13771

Ursodeoxycholic acid 25+ 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-13948A

Angiotensin II human acetate Maximum Cited Publications 222 Publications Verification Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate	Angiotensin Receptor Apoptosis	Cardiovascular Disease Infection Metabolic Disease Inflammation/Immunology 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-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt	Hepcidin Potassium Channel Endogenous Metabolite	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) .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor	Neurological Disease Metabolic Disease
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-15589

GW9508 5+ Cited Publications	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-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-14229

TGR5 Receptor Agonist 3 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-13771A

Ursodeoxycholic acid sodium 25+ 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-101483

Dihydromunduletone 2 Publications Verification	Drug Derivative	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 1 Publications Verification 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-N15721

Tryptophan-cholic acid Trp-CA	Orphan GPCR GLP Receptor	Metabolic Disease
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC₅₀=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .

HY-134494

MS48107 2 Publications Verification	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-113478S

Ursodeoxycholic acid-d4 Ursodeoxycholate-d₄; Ursodiol-d₄; UDCA-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 .

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-10499

PH-064 2 Publications Verification BIM-46187	Serotonin Transporter Akt	Neurological Disease Inflammation/Immunology Cancer
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 .

HY-W010516

2-Methylvaleric acid 2-Methylpentanoic acid	Endogenous Metabolite	Metabolic Disease
2-Methylvaleric acid is a branched short-chain fatty acid (SCFA) produced by the metabolism of branched-chain amino acids by gut microbes. 2-Methylvaleric acid can be used as a potential biomarker for metabolic diseases such as type 2 diabetes, and its content is significantly reduced in the feces of diabetic mice. 2-Methylvaleric acid may regulate host energy metabolism and inflammatory response through G protein-coupled receptors (GPCRs) or histone deacetylase (HDAC) inhibition. 2-Methylvaleric acid can be used to study gut microbe-host interactions and metabolic diseases as a fecal biomarker[1][2].

HY-13948B

Angiotensin II human TFA Maximum Cited Publications 222 Publications Verification Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA	Angiotensin Receptor Apoptosis	Cardiovascular Disease Metabolic Disease 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-153830

LacCer (d18:1/16:0) C16 Lactosylceramide (d18:1/16:0)	Endogenous Metabolite	Neurological Disease Metabolic Disease
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .

HY-47573

CCG273441 3 Publications Verification	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-13771R

Ursodeoxycholic acid (Standard) Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)	Reference Standards G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite	Infection Metabolic Disease Cancer
Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. 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-177116

GPR15 antagonist-1	HIV	Infection Inflammation/Immunology
GPR15 antagonist-1 (Compound 5) is a GPR15 antagonist. G protein-coupled receptor 15 (GPR15) is an extensively studied GPCRs involving HIV infection, colonic inflammation, and smoking-related diseases .

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-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-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-P10365

VPM-p15	Adhesion G Protein-coupled Receptors (AGPCRs)	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-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-113066AR

Guanosine 5'-diphosphate disodium salt (Standard) GDP disodium salt (Standard)	Hepcidin Endogenous Metabolite Potassium Channel Reference Standards	Neurological Disease Inflammation/Immunology Cancer
Guanosine 5'-diphosphate (disodium salt) (Standard) is the analytical standard of Guanosine 5'-diphosphate (disodium salt). This product is intended for research and analytical applications. 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-15589R

GW9508 (Standard)	Free Fatty Acid Receptor Potassium Channel Reference Standards	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 .

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-W783254

C18 LPA PA(18:0e/0:0)	G Protein-coupled Receptor Kinase (GRK) Calcium Channel	Cardiovascular Disease Cancer
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.

HY-14229R

TGR5 Receptor Agonist (Standard) CCDC (Standard)	G protein-coupled Bile Acid Receptor 1 Calcium Channel Reference Standards	Metabolic Disease
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 .

HY-W727728

MK-8666	Free Fatty Acid Receptor	Metabolic Disease
MK-8666 is a potent and selective partial GPR40 agonist (EC₅₀ = 0.54 nM for human GPR40). MK-8666 shows selectivity over GPR119, GPR43, GPR41, GPR120, and other G-protein-coupled receptors (GPCRs). MK-8666 reduces glucose in the rodent. MK-8666 can be used for type 2 diabetes research ^[1][2].

HY-P10289A

Neuropeptide W-30 (rat) acetate NPW30, rat acetate	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 .

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-153830S

LacCer (d18:1/16:0)-d3 C16 Lactosylceramide (d18:1/16:0)-d₃	Isotope-Labeled Compounds Endogenous Metabolite	Neurological Disease Metabolic Disease
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0))-d₃ is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. LacCer (d18:1/16:0) is also upregulated in a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder). LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .

HY-129118

Takeda103A	G Protein-coupled Receptor Kinase (GRK)	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-178978

α,δ-NAG	Drug Derivative Phosphatase ERK Ras	Inflammation/Immunology
α,δ-NAG is an orally active glutaminase-resistant less-hydrolyzable L-Glutamine derivative. α,δ-NAG is a G protein-coupled receptor (GPCR) allosteric modulator. α,δ-NAG suppresses neutrophilic airway inflammation by activating the *GPCR/ERK/MKP-1* pathway. α,δ-NAG can be used for the researches of inflammation and immunology, such as asthma .

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-160281

CCD-2	GCGR Adenosine Receptor	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-10499A

PH-064 (tetra(hydrochloride)) BIM-46187 tetrahydrochloride	Serotonin Transporter Akt	Neurological Disease Inflammation/Immunology Cancer
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 .

HY-P5084

Neuromedin S (human)	Neuromedin U Receptor (NMUR) G protein-coupled Bile Acid Receptor 1	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-W339834

1-Stearoyl-sn-glycerol 3-phosphate sodium	Acyltransferase Endogenous Metabolite Liposome	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-E70609

PIK3CG Recombinant Human Active Lipid Kinase	PI3K	Inflammation/Immunology Cancer
PIK3CG Recombinant Human Active Lipid Kinase belongs to PI3K enzyme family that is directly regulated by Gβγ and Ras in the G protein coupled receptor (GPCR) pathway. PIK3CG has the function of regulating cellular inflammation and immunity. PIK3CG is also a potential target for the treatment of a few malignant tumors such as acute lymphoblastic leukemia, medulloblastoma, claudin-low breast cancer (CLBC) and Kaposi sarcoma .

HY-W010516R

2-Methylvaleric acid (Standard) 2-Methylpentanoic acid (Standard)	Reference Standards Endogenous Metabolite	Metabolic Disease
2-Methylvaleric acid (Standard) is the analytical standard of 2-Methylvaleric acid. This product is intended for research and analytical applications. 2-Methylvaleric acid is a branched short-chain fatty acid (SCFA) produced by the metabolism of branched-chain amino acids by gut microbes. 2-Methylvaleric acid can be used as a potential biomarker for metabolic diseases such as type 2 diabetes, and its content is significantly reduced in the feces of diabetic mice. 2-Methylvaleric acid may regulate host energy metabolism and inflammatory response through G protein-coupled receptors (GPCRs) or histone deacetylase (HDAC) inhibition. 2-Methylvaleric acid can be used to study gut microbe-host interactions and metabolic diseases as a fecal biomarker[1][2].

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-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes .

HY-P11279

TC2	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC2 is an efficient GIPR-preferring monomeric quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.47, 2.1, 30, and 55 nM respectively. TC2 exhibits a significant GLP-1R preference, with a significant reduction in β-inhibitory protein 2 (βArr2) recruitment, while maintaining a strong cAMP signal. TC2 can be used for research on obesity and diabetes .

HY-101483R

Dihydromunduletone (Standard)	Drug Derivative Reference Standards	Neurological Disease Cancer
Dihydromunduletone (Standard) is the analytical standard of Dihydromunduletone (HY-101483). This product is intended for research and analytical applications. 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 .

Cat. No.	Product Name

HY-L006

GPCR/G Protein Compound Library

3,389 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 3,389 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

405 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 405 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

HY-L928

GPCR Targeted Diversity Library

7,113 compounds

G protein-coupled receptors (GPCRs) are membrane proteins in humans and one of the most important targets in drug discovery. Approximately 35% of launched drugs are targeted GPCRs, making them a crucial class of targets in drug discovery.

The orthosteric site of a GPCR is its endogenous ligand’s (such as neurotransmitters or hormones) binding site. This site plays a central role in signal transduction. Small molecules binding to this site typically contain a protonatable amino group, enabling the formation of salt bridges or hydrogen bonds with acidic residues in the binding pocket. In contrast, the allosteric site does not directly initiate signaling but modulates the signal intensity of the GPCR by altering or stabilizing the conformation of the orthosteric site. Small molecules binding to the allosteric site often contain multiple aromatic rings to occupy hydrophobic pockets and achieve their functional effects.

MCE has collected over 7,113 reported bioactive molecules targeting GPCRs, covering Class A, B, and C GPCRs. These small molecules were subjected to AI representation to extract 2D and 3D features. Subsequently, we do screening by AI score based on similarity to identify molecules in diversity library highly similar to the reported bioactive molecules in both 2D and 3D, with a threshold greater than 0.7. Further screening based on cLogP was applied to select molecules with good lipophilicity, which facilitates the binding of small molecules to GPCRs. This diversity library can be widely applied to the discovery of compounds targeting GPCR proteins.

HY-L013

Neuronal Signaling Compound Library

3,802 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 3,802 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-13948

Angiotensin II human Maximum Cited Publications 222 Publications Verification Angiotensin II; Ang II; DRVYIHPF	Angiotensin Receptor Apoptosis	Cardiovascular Disease Infection Metabolic Disease Inflammation/Immunology 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 222 Publications Verification Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate	Angiotensin Receptor Apoptosis	Cardiovascular Disease Infection Metabolic Disease Inflammation/Immunology 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 222 Publications Verification Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA	Angiotensin Receptor Apoptosis	Cardiovascular Disease Metabolic Disease 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-P10365

VPM-p15	Adhesion G Protein-coupled Receptors (AGPCRs)	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-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-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-P10289A

Neuropeptide W-30 (rat) acetate NPW30, rat acetate	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-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-P5084

Neuromedin S (human)	Neuromedin U Receptor (NMUR) G protein-coupled Bile Acid Receptor 1	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-P11275

TC4	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC4 is a highly balanced single-molecule quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.95, 31, 81, and 1100 nM respectively. TC4 exhibits extremely strong signal bias on GLP-1R and has very low recruitment efficacy for β-inhibitor protein 2 (βArr2) and this strong cAMP preference is believed to maximize metabolic benefits (such as weight loss and hypoglycemia) while possibly minimizing side effects mediated by β-inhibitor protein recruitment (such as receptor desensitization). TC4 can be used for research on obesity and diabetes .

HY-P11279

TC2	GLP Receptor GCGR Neuropeptide Y Receptor	Metabolic Disease
TC2 is an efficient GIPR-preferring monomeric quadruple agonist that can respectively activate GIPR, GLP-1R, GcgR, and Y2R with IC₅₀ values of 0.47, 2.1, 30, and 55 nM respectively. TC2 exhibits a significant GLP-1R preference, with a significant reduction in β-inhibitory protein 2 (βArr2) recruitment, while maintaining a strong cAMP signal. TC2 can be used for research on obesity and diabetes .

HY-P11133

Leukokinin 1	Peptides	Neurological Disease
Leukokinin 1 is a member of the leucokinin peptide family. Leukokinin 1 operates by binding to and activating specific G-protein-coupled receptors (GPCRs). Leukokinin 1 plays a wide role in the central nervous system (CNS) of molluscs. Leukokinin 1 can be used for research on neurological disease .

HY-P11156

Sulfated sulfakinin	Parasite	Infection
Sulfated sulfakinin is a *Sulfakinin receptor* (SKR) activator with EC₅₀*s of 1.6 and 5.4 nM for Tribolium castaneumTc* TcSKR1 and TcSKR2, respectively. SKRs are G-protein-coupled receptors (GPCRs) that interact with sulfakinins to modulate diverse biological processes. Sulfated sulfakinin can be used for tho control of pest insects research .

Cat. No.	Product Name	Target	Research Area	Image

HY-P991843

Anti-CCR5 Antibody (HEK/1/85a/7a)	CCR	Inflammation/Immunology
Anti-CCR5 Antibody (HEK/1/85a/7a) recognizes an epitope on human CCR5. CCR5 is a seven-transmembrane G-protein-coupled receptor (GPCR). Recommend Isotype Controls: Rat IgG2b kappa, Isotype Control (HY-P990682) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13948

Angiotensin II human Maximum Cited Publications 222 Publications Verification Angiotensin II; Ang II; DRVYIHPF	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Disease Research Fields Endocrinology Source Classification 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-13771

Ursodeoxycholic acid 25+ Cited Publications Ursodeoxycholate; Ursodiol; UDCA	Human Gut Microbiota Metabolites Other disease Classification of Application Fields Disease markers Endogenous metabolite Disease Research Fields Steroids Source Classification 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-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt	Structural Classification Natural Products Classification of Application Fields Endogenous metabolite Inflammation/Immunology Disease Research Fields Source Classification	Hepcidin Potassium Channel Endogenous Metabolite
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-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-13771A

Ursodeoxycholic acid sodium 25+ Cited Publications Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium	Microorganisms Classification of Application Fields Metabolic Disease Inflammation/Immunology Disease Research Fields Steroids Source Classification	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-N15721

Tryptophan-cholic acid Trp-CA	Triterpenes Structural Classification Terpenoids Endogenous metabolite Source Classification	Orphan GPCR GLP Receptor
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC₅₀=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .

HY-W010516

2-Methylvaleric acid 2-Methylpentanoic acid	other families Classification of Application Fields Ketones, Aldehydes, Acids Metabolic Disease Plants Endogenous metabolite Disease Research Fields Source Classification	Endogenous Metabolite
2-Methylvaleric acid is a branched short-chain fatty acid (SCFA) produced by the metabolism of branched-chain amino acids by gut microbes. 2-Methylvaleric acid can be used as a potential biomarker for metabolic diseases such as type 2 diabetes, and its content is significantly reduced in the feces of diabetic mice. 2-Methylvaleric acid may regulate host energy metabolism and inflammatory response through G protein-coupled receptors (GPCRs) or histone deacetylase (HDAC) inhibition. 2-Methylvaleric acid can be used to study gut microbe-host interactions and metabolic diseases as a fecal biomarker[1][2].

HY-153830

LacCer (d18:1/16:0) C16 Lactosylceramide (d18:1/16:0)	Microorganisms Saccharides Monosaccharides Source Classification	Endogenous Metabolite
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .

HY-13771R

Ursodeoxycholic acid (Standard) Ursodeoxycholate (Standard); Ursodiol (Standard); UDCA (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Other disease Disease markers Endogenous metabolite Steroids Source Classification	Reference Standards G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite
Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. 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-113066AR

Guanosine 5'-diphosphate disodium salt (Standard) GDP disodium salt (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Hepcidin Endogenous Metabolite Potassium Channel Reference Standards
Guanosine 5'-diphosphate (disodium salt) (Standard) is the analytical standard of Guanosine 5'-diphosphate (disodium salt). This product is intended for research and analytical applications. 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-W010516R

2-Methylvaleric acid (Standard) 2-Methylpentanoic acid (Standard)	Structural Classification other families Ketones, Aldehydes, Acids Plants Endogenous metabolite Source Classification	Reference Standards Endogenous Metabolite
2-Methylvaleric acid (Standard) is the analytical standard of 2-Methylvaleric acid. This product is intended for research and analytical applications. 2-Methylvaleric acid is a branched short-chain fatty acid (SCFA) produced by the metabolism of branched-chain amino acids by gut microbes. 2-Methylvaleric acid can be used as a potential biomarker for metabolic diseases such as type 2 diabetes, and its content is significantly reduced in the feces of diabetic mice. 2-Methylvaleric acid may regulate host energy metabolism and inflammatory response through G protein-coupled receptors (GPCRs) or histone deacetylase (HDAC) inhibition. 2-Methylvaleric acid can be used to study gut microbe-host interactions and metabolic diseases as a fecal biomarker[1][2].

Species:	Human (2) Mouse (1)
Tag:	His (3)
Source:	E. coli Cell-free (3)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P702301

	GPCR 20 variant Protein, Human (Cell-Free, His) G protein-coupled receptor 20 variant	Human	E. coli Cell-free
	GPCR 20 variant is a member of the G-protein coupled receptor 1 family. GPCR 20 variant Protein, Human (Cell-Free, His) is the recombinant human-derived GPCR 20 variant protein, expressed by E. coli Cell-free , with N-10*His labeled tag.

HY-P704194

	GPBAR1 Protein, Human (Cell-Free, His) G-protein coupled receptor GPCR19; hGPCR19; Membrane-type receptor for bile acids; M-BAR; hBG37; BG37; GPBAR1; TGR5	Human	E. coli Cell-free
	GPBAR1 Protein, Human (Cell-Free, His) is the recombinant human-derived GPBAR1 protein, expressed by E. coli cell-free system, with N-10*His tag.

HY-P705541

	S1pr2 Protein, Mouse (Cell-Free, His) Sphingosine 1-phosphate receptor 2; S1P receptor 2; S1P2; Endothelial differentiation G-protein coupled receptor 5; Lysophospholipid receptor B2; Sphingosine 1-phosphate receptor Edg-5 (S1P receptor Edg-5); Edg5; Gpcr13; Lpb2	Mouse	E. coli Cell-free

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Cat. No.	Product Name	Chemical Structure

HY-113478S

Ursodeoxycholic acid-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 .

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 .

HY-153830S

LacCer (d18:1/16:0)-d3

LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0))-d₃ is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. LacCer (d18:1/16:0) is also upregulated in a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder). LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .

Host:	Rabbit (5)
Reactivity:	Human (5) Rat (3) Mouse (4)
Application:	IHC-P (2) ICC/IF (4) IF-Tissue (1) WB (4) IHC-F (2) FC (3) ELISA (2)
Isotype:	IgG (5)
Conjugation:	Non-conjugated (5)
Clonality:	Polyclonal (2) Monoclonal (3) Recombinant (2)
Modification:	Unmodified (5)

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HY-P81225

	GPR43 Antibody GPCR GPR43; FFA2R; Ffar2; FFAR2_HUMAN; free fatty acid activated receptor 2; Free fatty acid receptor 2; G protein coupled receptor 43; G protein-coupled receptor 43; G-protein coupled receptor 43; GPR 43; GPCR 43.	IHC-P, IHC-F, ICC/IF, ELISA, IF-Tissue	Human, Mouse
	GPR43 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to GPR43.

HY-P86697

	GPR84 Antibody (YA6389) G protein coupled receptor 84; G-protein coupled receptor 84; G protein coupled receptor EX33; GPCR 4; GPCR4; GPR 84; GPR84_HUMAN; GPR84(EX33); EX33; Inflammation related G protein coupled receptor EX33; Inflammation-related G-protein coupled receptor EX33; GPCR EX33; EX 33; GPCR GPR84;	WB	Human
	GPR84 Antibody (YA6389) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to GPR84.

HY-P81150

	GPR30 Antibody 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.	WB, IHC-P, IHC-F, ICC/IF, FC, ELISA	Human, Mouse, Rat
	GPR30 Antibody is a Rabbit-derived and non-conjugated IgG polyclonal antibody, targeting to GPR30.

HY-P82956

	HRH3 Antibody (YA2701) HRH3; GPCR97; Histamine H3 receptor; H3R; HH3R; G-protein coupled receptor 97	WB, ICC/IF, FC	Human, Mouse, Rat
	HRH3 Antibody (YA2701) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to HRH3.

HY-P87577

	OXGR1/GPR80 Antibody (YA7261) 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	WB, FC, ICC/IF	Human, Mouse, Rat
	OXGR1/GPR80 Antibody (YA7261) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to OXGR1/GPR80.

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Cat. No.	Product Name		Classification

HY-113066A

Guanosine 5'-diphosphate disodium salt 2 Publications Verification GDP disodium salt		Nucleotide 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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