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Results for "

G-protein Activator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Acyltransferase (1) Adenosine Receptor (1) Adhesion G Protein-coupled Receptors (AGPCRs) (1) Adrenergic Receptor (2) Angiotensin-converting Enzyme (ACE) (2) Apelin Receptor (APJ) (3) Aryl Hydrocarbon Receptor (3) Bombesin Receptor (1) Cannabinoid Receptor (3) CD3 (1) Cholinesterase (ChE) (1) Complement System (2) CXCR (2) DNA/RNA Synthesis (2) Drug Metabolite (2) Endogenous Metabolite (24) ERK (4) Estrogen Receptor/ERR (2) Free Fatty Acid Receptor (1) FXR (4) G protein-coupled Bile Acid Receptor 1 (12) GLP Receptor (1) GLUT (1) GPR171 (1) GPR35 (1) GPR55 (2) Isotope-Labeled Compounds (4) Kisspeptin Receptor (1) Liposome (1) mAChR (4) Mas-related G-protein-coupled Receptor (MRGPR) (3) MEK (1) MicroRNA (1) Neuropeptide B/W Receptor (2) Neuropeptide Y Receptor (2) Neurotensin Receptor (3) NF-κB (1) Opioid Receptor (8) Orexin Receptor (OX Receptor) (4) Orphan Receptor (1) Oxytocin Receptor (2) p38 MAPK (1) Phosphodiesterase (PDE) (1) Phospholipase (1) PKC (3) Platelet-activating Factor Receptor (PAFR) (2) Potassium Channel (3) Protease Activated Receptor (PAR) (3) TNF Receptor (1) Trace Amine-associated Receptor (TAAR) (2) Transmembrane Glycoprotein (1) Vasopressin Receptor (2) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (20) Cardiovascular Disease (8) Endocrinology (12) Infection (4) Inflammation/Immunology (17) Metabolic Disease (21) Neurological Disease (37)
Oligonucleotides:	Nucleotides and their Analogs (4) Emulsifiers (1) Phospholipids (2)

Inhibitors & Agonists

Screening Libraries

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P5985

mSIRK 1 Publications Verification	ERK	Others
mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC₅₀ of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .

HY-137677B

GTPγS tetralithium Guanosine 5'-[γ-thio]triphosphate tetralithium	GLUT	Others
GTPγS (tetralithium) (Guanosine 5'-[γ-thio]triphosphate (tetralithium)) is a G-protein activator that protects proteins from proteolytic degradation, stimulates GLUT4 translocation in a tyrosine kinase-dependent manner, stimulate phospholipases and induce actin polymerization. GTPγS (tetralithium) to couple with G- protein α, to study its effect on kinase activity. GTPγS (tetralithium) acts as a component of lysis buffer .

HY-P0195

Bombesin 1 Publications Verification	Bombesin Receptor	Neurological Disease Metabolic Disease
Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors .

HY-P1376A

G-Protein antagonist peptide TFA	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

HY-P1944A

Apelin-13 TFA 5+ Cited Publications	Apelin Receptor (APJ)	Cardiovascular Disease Metabolic Disease
Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC₅₀ value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome .

HY-115768

Compound 48/80 Poly-p-methoxyphenethylmethylamine	Phospholipase	Neurological Disease Cancer
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .

HY-P1376

G-Protein antagonist peptide	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of G_i or G_o and inhibits G_s activation by β-adrenoceptors.

HY-P1944

Apelin-13	Apelin Receptor (APJ)	Cardiovascular Disease Metabolic Disease
Apelin-13 is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC₅₀ value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome .

HY-163277

PIPE-3297	Opioid Receptor	Inflammation/Immunology
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

HY-117403

AB-FUBICA	Cannabinoid Receptor Potassium Channel
AB-FUBICA (Compound 13) is a CB1 and CB2 receptor agonist that activates G-protein coupled inwardly rectifying potassium channels (GIRK) by binding to CB1 and CB2 receptors, displaying notable cannabinoid-like activity. AB-FUBICA has EC₅₀ values of 21 nM for CB1 and 15 nM for CB2. AB-FUBICA may be suitable for studying pain management, neurodegenerative diseases, and inflammation-related mechanisms .

HY-13771A

Ursodeoxycholic acid sodium 15+ 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-P2705

Mastoparan X	Endogenous Metabolite	Others
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of *G protein* that couple to phospholipase C to cause secretion from various kinds of cells .

HY-170973

KOR agonist 4	Opioid Receptor
KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC₅₀ of 14 nM and with an E_max of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .

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-13771

Ursodeoxycholic acid 15+ 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-N0593

Deoxycholic acid 10+ Cited Publications Cholanoic Acid; Desoxycholic acid	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-N0593A

Deoxycholic acid sodium salt 10+ Cited Publications Sodium deoxycholate	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid sodium salt (sodium deoxycholate), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-N0593B

Deoxycholic acid sodium hydrate Cholanoic Acid sodium hydrate; Desoxycholic acid sodium hydrate	Endogenous Metabolite G protein-coupled Bile Acid Receptor 1	Metabolic Disease
Deoxycholic acid (cholanoic acid) sodium hydrate, a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-164795

SBI-810	Neurotensin Receptor	Neurological Disease
SBI-810 is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .

HY-164795A

SBI-810 hydrochloride	Neurotensin Receptor	Neurological Disease
SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12 .

HY-13771R

Ursodeoxycholic acid (Standard)	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-P5372

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2	Protease Activated Receptor (PAR)	Others
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)

HY-12695B

Guanosine 5'-triphosphate trisodium salt hydrate 5+ Cited Publications 5'-GTP trisodium salt hydrate	Endogenous Metabolite DNA/RNA Synthesis	Others
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.

HY-16642A

LY2828360	Cannabinoid Receptor	Neurological Disease
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB₂) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.

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-115575

tBPC	Neuropeptide Y Receptor	Metabolic Disease
tBPC is a selective positive allosteric modulator for human Y4 receptor (Y4R), which enhances the activation of Y4R in G protein signaling and arrestin3 recruitment .

HY-N0593S1

Deoxycholic acid-d5	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid-d₅ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-N0593S

Deoxycholic acid-d4	Isotope-Labeled Compounds G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid-d₄ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-N0593S2

Deoxycholic acid-d6 Cholanoic Acid-d₆; Desoxycholic acid-d₆	Isotope-Labeled Compounds G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid-d₆ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-N0593R

Deoxycholic acid (Standard) Cholanoic Acid(Standard); Desoxycholic acid (Standard)	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid (Standard) is the analytical standard of Deoxycholic acid. This product is intended for research and analytical applications. Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-101108R

Tazarotenic acid (Standard)	Drug Metabolite	Others
Deoxycholic acid (Standard) is the analytical standard of Deoxycholic acid. This product is intended for research and analytical applications. Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-N0593S3

Deoxycholic acid-13C Cholanoic Acid-¹³C; Desoxycholic acid-¹³C	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite	Metabolic Disease
Deoxycholic acid- ¹³C is the ¹³C-labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-122203

PCS1055 dihydrochloride 2 Publications Verification	mAChR Cholinesterase (ChE)	Neurological Disease
PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC₅₀ of 18.1 nM and a K_d of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ ³H]-NMS binding to the M4 receptor with a K_i of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC₅₀ s of 22 nM and 120 nM for electric eel and human AChE, respectively .

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) .

HY-P1318

Ac-RYYRIK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P1318A

Ac-RYYRIK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P10716

Exendin-P5	GLP Receptor	Metabolic Disease
Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in *G protein*-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .

HY-118086

MRS1067	Adenosine Receptor	Inflammation/Immunology Cancer
MRS 1067 is a competitive antagonist of the adenosine A3 receptor that inhibits the suppression of adenylate cyclase by adenosine A3 receptor agonists and affects the activation of *G proteins*. MRS 1067 can be used in research related to inflammation and cancer .

HY-159177

M4 mAChR Modulator-1	mAChR	Neurological Disease
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .

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-159923

BPRMU191	Opioid Receptor	Neurological Disease
BPRMU191 is a μ-opioid receptor (MOR) modulator that converts small-molecule morphinan antagonists into G protein-biased MOR agonists, thereby inducing MOR-dependent activation and analgesic effects. Co-administration of BPRMU191 with morphinan antagonists provides analgesia while reducing side effects such as gastrointestinal dysfunction, antinociceptive tolerance, and dependency-related adverse effects. BPRMU191, in combination with morphinan antagonists, offers a potential strategy for studying severe pain management and G protein-coupled receptor modulation .

HY-138121

PSB-KD107	Cannabinoid Receptor	Inflammation/Immunology
PSB-KD107 is an agonist of the cannabinoid activated orphan G-protein-coupled receptor GPR18, and PSB-KD107 has anti-inflammatory activity. PSB-KD107 can be used in the study of Duchenne muscular dystrophy .

HY-P5213

Vasopressin Dimer (parallel) (TFA)	Vasopressin Receptor Oxytocin Receptor	Endocrinology
Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .

HY-114164C

Thrombin, Pig blood	Protease Activated Receptor (PAR)	Inflammation/Immunology
Thrombin, Pig blood is a key enzyme in the coagulation cascade, responsible for converting fibrinogen into fibrin. Thrombin, Pig blood activates platelet activation, endothelial cell function, and inflammatory responses by binding to PAR-1 and PAR-4, which triggers G protein-coupled signaling pathways. Thrombin, Pig blood holds promise for research in coagulation and inflammation fields .

HY-112384B

DL-threo-Dihydrosphingosine	ERK	Inflammation/Immunology
DL-threo-Dihydrosphingosine is a extracellular signal-regulated kinase(ERK) signalling cassette inhibitor and is effective against both growth factor- and G-protein-dependent activation of ERK. DL-threo-Dihydrosphingosine inhibits smooth muscle cell proliferation and can be used for study of asthma .

HY-P3843

Neuropeptide AF (cattle)	Mas-related G-protein-coupled Receptor (MRGPR) Neuropeptide Y Receptor	Neurological Disease
Neuropeptide AF (cattle), an amidated octadecapeptide, is RFamide neuropeptide. Neuropeptide AF (cattle) acts as a ligand of Mas-related gene receptor A4 (MrgprA4) (*Mas-related G-protein-coupled Receptor (MRGPR)) (EC₅₀* of ~60 nM) and MrgprC11 (EC₅₀ of ~300 nM). Neuropeptide AF (cattle) also activate to the G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) (EC₅₀ of ~25-325 nM) and NPFF2 (EC₅₀ of ~1-5 nM). Neuropeptide AF (cattle) shows anti-opiate and related pain modulation effects .

HY-108635

C16-PAF Maximum Cited Publications 24 Publications Verification PAF (C16)	p38 MAPK MEK ERK Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability .

HY-B1816

Zaprinast 2 Publications Verification M&B 22948	Phosphodiesterase (PDE) GPR35	Cardiovascular Disease Neurological Disease Endocrinology
Zaprinast (M&B 22948) is a selective inhibitor of cGMP-selective Phosphodiesterase (PDE5). Zaprinast causes a significant increase in cGMP levels in myocytes. Zaprinast is a G protein-coupled receptor 35 (GPR35) agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects .

HY-P1803

Protein Kinase C Peptide Substrate PKCε; PRKCE ; Peptide Epsilon	PKC	Neurological Disease Inflammation/Immunology Endocrinology
Protein Kinase C Peptide Substrate is targeted to a specific cellular compartment in a manner dependent on second messengers and on specific adapter proteins in response to extracellular signals that activate G-protein-coupled receptors, tyrosine kinase receptors, or tyrosine kinase-coupled receptors. Protein Kinase C Peptide Substrate then regulates various physiological functions including the activation of nervous, endocrine, exocrine, inflammatory, and immune systems .

Cat. No.	Product Name

HY-L120

GABA Receptor Compound Library

165 compounds

GABA receptors are a class of receptors that respond to the neurotransmitter gamma-aminobutyric acid (GABA), the chief inhibitory neurotransmitter in the vertebrate central nervous system. There are two classes of GABA receptors: GABAA and GABAB. GABAA receptors are ligand-gated ion channels (also known as ionotropic receptors), whereas GABAB receptors are G protein-coupled receptors (also known asmetabotropic receptors). GABA receptors are significant drug targets in the treatment of neuropsychiatric disorders such as epilepsy, insomnia, and anxiety, as well as in anesthesia in surgical operations.

MCE offers a unique collection of 165 GABA receptors inhibitors and activators, which is an efficient tool for neuropsychiatric disorders drugs discovery.

HY-L006

GPCR/G Protein Compound Library

2,921 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 2,921 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.

HY-L132

Chemokine Compound Library

188 compounds

Chemokines, or chemotactic cytokines, are small cytokines or signaling proteins secreted by cells. They are a component of intercellular communication, controlling the directional movement of immune cells especially leukocytes, as well as other cell types, for instance, endothelial and epithelial cells, which are essential to maintain human health and the function of the immune system.

The biological effects of chemokines are achieved by binding to chemokine receptors, which are G protein-coupled receptors found on the surface of leukocytes. Some chemokine receptors are involved in directing tumor metastasis and over-expression by certain tumors. So inhibiting the interaction between chemokine and chemokine receptors on the surface of tumor cells may be a new possible therapeutic approach. Some chemokine receptors are coreceptors for HIV entry, and related inhibitors have been approved by the FDA to treat patients with HIV. Obviously, chemokines and chemokine receptors have become new targets for studying cancer, HIV, inflammation, and other diseases.

MCE supplies a unique collection of 188 chemokine or chemokine receptor inhibitors and activators, all of which have the identified inhibitory or activated effect on chemokine or chemokine receptors. MCE Chemokine Library is a useful tool for drug research related to cancer, AIDS, and wound therapy.

HY-L121

5-HT Receptor Compound Library

350 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 350 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Target	Research Area

HY-P5985

mSIRK 1 Publications Verification	ERK	Others
mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC₅₀ of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .

HY-P0195

Bombesin 1 Publications Verification	Bombesin Receptor	Neurological Disease Metabolic Disease
Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors .

HY-P1376A

G-Protein antagonist peptide TFA	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide TFA is a truncated substance P-related peptide, competes with receptor for G protein binding. G-Protein antagonist peptide TFA inhibits the activation of G_i or G_o by M2 muscarinic cholinergic receptor (M2 mAChR) or of G_s by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .

HY-P1944A

Apelin-13 TFA 5+ Cited Publications	Apelin Receptor (APJ)	Cardiovascular Disease Metabolic Disease
Apelin-13 TFA is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC₅₀ value of 0.37 nM. Apelin-13 TFA has vasodilatory and antihypertensive effects. Apelin-13 TFA also can be used for researching type 2 diabetes and metabolic syndrome .

HY-P2705

Mastoparan X	Endogenous Metabolite	Others
Mastoparan X is a GTP-binding regulatory protein (G protein)-activating peptide, and a tetradecapeptide from wasp venom. Mastoparan X acts function by the direct activation of *G protein* that couple to phospholipase C to cause secretion from various kinds of cells .

HY-P1376

G-Protein antagonist peptide	mAChR Adrenergic Receptor	Endocrinology
G-Protein antagonist peptide is the substance P-related peptide that inhibits binding of G proteins to their receptors. G-Protein antagonist peptide competitively and reversibly inhibits M2 muscarinic receptor activation of G_i or G_o and inhibits G_s activation by β-adrenoceptors.

HY-P1944

Apelin-13	Apelin Receptor (APJ)	Cardiovascular Disease Metabolic Disease
Apelin-13 is an endogenous ligand for the G-protein coupled receptor angiotensin II protein J (APJ), activating this G protein-coupled receptor with an EC₅₀ value of 0.37 nM. Apelin-13 is widely distributed in the central and peripheral nervous systems. Apelin-13 has vasodilatory and antihypertensive effects. Apelin-13 also can be used for researching type 2 diabetes and metabolic syndrome .

HY-P5372

Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2	Protease Activated Receptor (PAR)	Others
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)

HY-P1318

Ac-RYYRIK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P1318A

Ac-RYYRIK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ ³⁵S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .

HY-P10716

Exendin-P5	GLP Receptor	Metabolic Disease
Exendin-P5 is a selective agonist that targets the GLP-1R. Exendin-P5 promotes rapid activation of G proteins by transient interactions with the transmembrane domain of GLP-1R, enhancing its potency in *G protein*-mediated signaling and accelerating cAMP production. This mechanism suggests the potential application of Exendin-P5 in the study of metabolic diseases .

HY-P5213

Vasopressin Dimer (parallel) (TFA)	Vasopressin Receptor Oxytocin Receptor	Endocrinology
Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .

HY-P3843

Neuropeptide AF (cattle)	Mas-related G-protein-coupled Receptor (MRGPR) Neuropeptide Y Receptor	Neurological Disease
Neuropeptide AF (cattle), an amidated octadecapeptide, is RFamide neuropeptide. Neuropeptide AF (cattle) acts as a ligand of Mas-related gene receptor A4 (MrgprA4) (*Mas-related G-protein-coupled Receptor (MRGPR)) (EC₅₀* of ~60 nM) and MrgprC11 (EC₅₀ of ~300 nM). Neuropeptide AF (cattle) also activate to the G protein-coupled receptors NPFF1 (Neuropeptide Y Receptor) (EC₅₀ of ~25-325 nM) and NPFF2 (EC₅₀ of ~1-5 nM). Neuropeptide AF (cattle) shows anti-opiate and related pain modulation effects .

HY-P1803

Protein Kinase C Peptide Substrate PKCε; PRKCE ; Peptide Epsilon	PKC	Neurological Disease Inflammation/Immunology Endocrinology
Protein Kinase C Peptide Substrate is targeted to a specific cellular compartment in a manner dependent on second messengers and on specific adapter proteins in response to extracellular signals that activate G-protein-coupled receptors, tyrosine kinase receptors, or tyrosine kinase-coupled receptors. Protein Kinase C Peptide Substrate then regulates various physiological functions including the activation of nervous, endocrine, exocrine, inflammatory, and immune systems .

HY-P5214

Vasopressin Dimer (anti-parallel) (TFA)	Vasopressin Receptor Oxytocin Receptor	Endocrinology
Vasopressin Dimer (anti-parallel) TFA is an anti-parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (anti-parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR .

HY-P2210A

BigLEN(mouse) TFA	GPR171	Neurological Disease
BigLEN(mouse) TFA is a GPR171 agonist. BigLEN(mouse) TFA is a proSAAS-derived neuropeptide. BigLEN(mouse) TFA regulates food intake in mice. BigLEN(mouse) inhibits the release of glutamate onto parvocellular neurons of the paraventricular nucleus in a process dependent upon activation of postsynaptic G proteins.

HY-P2544

[Lys8, Lys9]-Neurotensin (8-13) JMV438	Neurotensin Receptor	Neurological Disease
[Lys8, Lys9]-Neurotensin (8-13) (JMV438), a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with K_i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively .

HY-P1241

BAM(8-22)	Mas-related G-protein-coupled Receptor (MRGPR)	Neurological Disease Inflammation/Immunology
BAM(8-22), a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) has an analgesic effect and can also inhibit the activation of microglia .

HY-P1241A

BAM(8-22) TFA	Mas-related G-protein-coupled Receptor (MRGPR)	Neurological Disease Inflammation/Immunology
BAM(8-22) TFA, a proteolytically cleaved product of proenkephalin A and sensory neuron-specific receptor (SNSR) agonist, is a potent activator of Mas-related G-protein-coupled receptors (Mrgprs), MrgprC11 and hMrgprX1. BAM(8-22) TFA induces scratching in mice in an Mrgpr-dependent manner. In addition, BAM(8-22) TFA has an analgesic effect and can also inhibit the activation of microglia .

HY-P0172

ATI-2341	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P0172A

ATI-2341 TFA 2 Publications Verification	CXCR	Inflammation/Immunology Endocrinology Cancer
ATI-2341 is a potent and functionally selective allosteric agonist of C-X-C chemokine receptor type 4 (CXCR4), which functions as a biased ligand, favoring Gαi activation over Gα13. ATI-2341 activates the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization. ATI-2341 is a potent and efficacious mobilizer of bone marrow polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) .

HY-P10495

GPR110 peptide agonist P12	Transmembrane Glycoprotein	Others Cancer
GPR110 peptide agonist P12 is a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 can be used in the study of developmental disorders and cancers related to GPR110 .

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-P10489

Kisspeptin-14 human	Kisspeptin Receptor	Others Cancer
Kisspeptin-14 human is a peptide hormone encoded by the KiSS-1 gene. Kisspeptin-14 human, along with several other similar peptide hormones, is produced from a common precursor protein by cleavage by different proteases. Kisspeptin-14 human has the same receptor binding efficiency and potency as full-length kisspeptin. Kisspeptin-14 human binds to its receptor GPR54 and is able to activate this G protein-coupled receptor and activate multiple intracellular signaling pathways. Kisspeptin-14 human can be used to study reproductive development and tumor metastasis .

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-106224B

Orexin A (human, rat, mouse) (acetate) Maximum Cited Publications 8 Publications Verification Hypocretin-1 (human, rat, mouse) (acetate)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (Hypocretin-1) (human, rat, mouse) acetate is a hypothalamic neuropeptide with analgesic properties (crosses the blood-brain barrier). Orexin A (human, rat, mouse) acetate binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) acetate can be used in studies of appetite regulation, neurodegenerative diseases and modulation of injurious messaging .

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-P1349A

Orexin B, rat, mouse TFA Rat orexin B TFA; Orexin B (mouse) TFA	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
Orexin B, rat, mouse (Rat orexin B) TFA is an endogenous orexin receptor agonist. Orexin B, rat, mouse TFA binds and activates two closely related orphan G protein-coupled receptors OX1-R and OX2-R. Orexin B, rat, mouse TFA stimulates food intake and energy expenditure and plays a significant role in sleep-wakefulness regulation .

HY-P10495A

GPR110 peptide agonist P12 acetate	Peptides	Cancer
GPR110 peptide agonist P12 acetate is the acetate salt form of GPR110 peptide agonist P12 (HY-P10495). GPR110 peptide agonist P12 acetateis a peptide that acts as a GPR110 agonist. GPR110 peptide agonist P12 acetate can significantly enhance the initial rate of GPR110 stimulated G protein GTPγS binding. GPR110 peptide agonist P12 acetate mimics the action of natural ligands, causing the extracellular domain (ECD) of the GPR110 to dissociate from the seven transmembrane domains (7TM), exposing the β-strand-13/stalk region at the N-terminus of the 7TM domain, which acts as an agonist to activate G protein signaling. GPR110 peptide agonist P12 acetate can be used in the study of developmental disorders and cancers related to GPR110 .

HY-107146

PZ-128 P1pal-7	Protease Activated Receptor (PAR)	Cardiovascular Disease Cancer
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible *protease-activated* receptor-1 (PAR1)** antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .

HY-P1345

TLQP-21	Complement System	Neurological Disease Endocrinology
TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca ²⁺. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions .

HY-106224

Orexin A (human, rat, mouse) Maximum Cited Publications 8 Publications Verification Hypocretin-1 (human, rat, mouse)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .

HY-P1345A

TLQP-21 TFA 1 Publications Verification	Complement System	Neurological Disease Endocrinology
TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC₅₀: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca ²⁺. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions .

HY-106224A

Orexin A (human, rat, mouse) (TFA) Maximum Cited Publications 8 Publications Verification Hypocretin-1 (human, rat, mouse) (TFA)	Orexin Receptor (OX Receptor)	Neurological Disease
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .

Cat. No.	Product Name	Target	Research Area

HY-P99394

Talquetamab JNJ-64407564	CD3	Cancer
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-P0195

Bombesin 1 Publications Verification	Structural Classification Natural Products Animals Source classification	Bombesin Receptor
Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors .

HY-13771A

Ursodeoxycholic acid sodium 15+ 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 15+ 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-N0593

Deoxycholic acid 10+ Cited Publications Cholanoic Acid; Desoxycholic acid	Structural Classification Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Steroids	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite
Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-N0593A

Deoxycholic acid sodium salt 10+ Cited Publications Sodium deoxycholate	Structural Classification Microorganisms Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Steroids	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite
Deoxycholic acid sodium salt (sodium deoxycholate), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-12695B

Guanosine 5'-triphosphate trisodium salt hydrate 5+ Cited Publications 5'-GTP trisodium salt hydrate	Structural Classification Natural Products Classification of Application Fields Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite DNA/RNA Synthesis
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.

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) .

HY-108635

C16-PAF Maximum Cited Publications 24 Publications Verification PAF (C16)	Structural Classification Natural Products Human Gut Microbiota Metabolites Classification of Application Fields Source classification Endogenous metabolite Inflammation/Immunology Disease Research Fields	p38 MAPK MEK ERK Endogenous Metabolite
C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability .

HY-13771R

Ursodeoxycholic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Other disease Source classification Disease markers Endogenous metabolite Steroids	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-N0593R

Deoxycholic acid (Standard) Cholanoic Acid(Standard); Desoxycholic acid (Standard)	Structural Classification Human Gut Microbiota Metabolites Microorganisms Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields Steroids	G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite
Deoxycholic acid (Standard) is the analytical standard of Deoxycholic acid. This product is intended for research and analytical applications. Deoxycholic acid (cholanoic acid), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-W010737

Guanosine-5'-triphosphate disodium salt 5+ Cited Publications 5'-GTP disodium salt	Structural Classification Natural Products Classification of Application Fields Source classification Metabolic Disease Endogenous metabolite Disease Research Fields	Endogenous Metabolite MicroRNA
Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration .

HY-12695

Guanosine 5'-triphosphate trisodium salt 5+ Cited Publications 5'-GTP trisodium salt	Structural Classification Classification of Application Fields Ketones, Aldehydes, Acids Source classification Other Diseases Endogenous metabolite Disease Research Fields	Endogenous Metabolite DNA/RNA Synthesis
Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration .

HY-W014502

D-Kynurenine	Classification of Application Fields Ketones, Aldehydes, Acids Source classification Endogenous metabolite Disease Research Fields Cancer	Aryl Hydrocarbon Receptor Endogenous Metabolite
D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR) .

HY-141581

Lyso-PAF C-18	Cardiovascular Disease Structural Classification Natural Products Classification of Application Fields Source classification Endogenous metabolite Disease Research Fields	Platelet-activating Factor Receptor (PAFR) Endogenous Metabolite
Lyso-PAF C-18 is an intermediate for the synthesis of C18-PAF (HY-130345). It has an easily substituted "Lyso-PAF" structure and is easy to purify and has high yield. C18-PAF is a ligand for platelet-activating factor and PAF G protein-coupled receptor (PAFR) and has renovasodilator properties and antihypertensive lipid properties .

HY-W014502R

D-Kynurenine (Standard)	Structural Classification Ketones, Aldehydes, Acids Endogenous metabolite	Aryl Hydrocarbon Receptor Endogenous Metabolite
D-Kynurenine (Standard) is the analytical standard of D-Kynurenine. This product is intended for research and analytical applications. D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR) .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Structural Classification 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 .

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-N0593S1

Deoxycholic acid-d5
Deoxycholic acid-d₅ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-N0593S

Deoxycholic acid-d4
Deoxycholic acid-d₄ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

HY-N0593S3

Deoxycholic acid-13C
Deoxycholic acid- ¹³C is the ¹³C-labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

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].

HY-N0593S2

Deoxycholic acid-d6
Deoxycholic acid-d₆ is the deuterium labeled Deoxycholic acid. Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.

Cat. No.	Product Name		Classification

HY-N0593A

Deoxycholic acid sodium salt Maximum Cited Publications 15 Publications Verification Sodium deoxycholate		Emulsifiers
Deoxycholic acid sodium salt (sodium deoxycholate), a bile acid, is a by-product of intestinal metabolism, that activates the G protein-coupled bile acid receptorTGR5 .

HY-12695B

Guanosine 5'-triphosphate trisodium salt hydrate 5+ Cited Publications 5'-GTP trisodium salt hydrate		Nucleotides and their Analogs
5'-GTP trisodium salt hydrate is an activator of the signal transducing G proteins and also serves as an energy-rich precursor of mononucleotide units in the enzymatic biosynthesis of DNA and RNA.

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-W010737

Guanosine-5'-triphosphate disodium salt 5+ Cited Publications 5'-GTP disodium salt		Nucleotides and their Analogs
Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration .

HY-12695

Guanosine 5'-triphosphate trisodium salt 5+ Cited Publications 5'-GTP trisodium salt		Nucleotides and their Analogs
Guanosine 5'-triphosphate (5'-GTP) trisodium salt is a G protein (G proteins) signaling activator and a high-energy precursor in the biosynthesis of nucleotide units in DNA and RNA. Guanosine 5'-triphosphate trisodium salt can promote myogenic cell differentiation by upregulating miRNA (miR133a, miR133b) and myogenic regulatory factor expression, and by inducing human myogenic precursor cells to release exosomes containing guanosine molecules. Guanosine-5'-triphosphate disodium salt holds promise for research in biosynthesis and skeletal muscle regeneration .

HY-130345

PAF (C18)		Phospholipids
C18-PAF, octadecane PAF, is the ligand of platelet-activating factor and PAF G protein-coupled receptor (PAFR). C18-PAF has renovasodilator properties and antihypertensive lipid properties. C18-PAF increases renal blood flow and causes dose-dependent systemic hypotension .

HY-W355700

1-Oleoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine		Phospholipids
1-oleoyl-sn-glycero-3-phosphoethanolamine (LysoPE 18:1) is a lysophosphatidylethanolamine molecule involved in phospholipid metabolism, targeting cell membrane receptors (such as G protein-coupled receptors) to regulate cell signaling pathways. 1-oleoyl-sn-glycero-3-phosphoethanolamine may activate mitogen-activated protein kinase (MAPK) signaling, promote cell migration, regulate inflammatory responses and lipid metabolism, and has both pro-inflammatory and anti-inflammatory activities. 1-oleoyl-sn-glycero-3-phosphoethanolamine is mainly used in the screening of biomarkers for metabolic diseases (such as non-alcoholic fatty liver disease and obesity), as well as the study of the mechanism of lysophospholipids in cell membrane homeostasis and signal transduction .

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