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G-protein Activator

" in MedChemExpress (MCE) Product Catalog:

114

Inhibitors & Agonists

4

Screening Libraries

37

Peptides

1

Inhibitory Antibodies

20

Natural
Products

7

Isotope-Labeled Compounds

1

Click Chemistry

11

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P5985
    mSIRK
    2 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 .
    mSIRK
  • 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 .
    GTPγS tetralithium
  • 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 .
    Bombesin
  • 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 Gi or Go by M2 muscarinic cholinergic receptor (M2 mAChR) or of Gs by beta-adrenergic receptor in the reconstituted phospholipid vesicles, assayed by receptor-promoted GTP hydrolysis .
    G-Protein antagonist peptide TFA
  • 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 EC 50 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 .
    Apelin-13 TFA
  • HY-115768
    Compound 48/80
    1 Publications Verification

    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 .
    Compound 48/80
  • HY-P1944
    Apelin-13
    5+ Cited Publications

    		 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 EC 50 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 .
    Apelin-13
  • 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 Gi or Go and inhibits Gs activation by β-adrenoceptors.
    G-Protein antagonist peptide
  • HY-174728
    Human CXCR1 mRNA

    		mRNA Inflammation/Immunology
    Human CXCR1 mRNA encodes the human C-X-C motif chemokine receptor 1 (CXCR1) protein, a member of the G-protein-coupled receptor family. CXCR1 is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system.
    Human CXCR1 mRNA
  • HY-175099
    AB-ICA

    		Drug Intermediate Neurological Disease
    AB-ICA is a precursor of AB-FUBICA (HY-117403). 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-ICA
  • 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 .
    PIPE-3297
  • HY-174727
    Human CXCR2 mRNA

    		mRNA Inflammation/Immunology
    Human CXCR2 mRNA encodes the human C-X-C motif chemokine receptor 2 (CXCR2) protein, a member of the G-protein-coupled receptor family. CXCR2 is a receptor for interleukin 8 (IL8). It binds to IL8 with high affinity, and transduces the signal through a G-protein activated second messenger system. This receptor also binds to chemokine (C-X-C motif) ligand 1 (CXCL1/MGSA), a protein with melanoma growth stimulating activity, and has been shown to be a major component required for serum-dependent melanoma cell growth.
    Human CXCR2 mRNA
  • 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 .
    AB-FUBICA
  • 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 .
    Ursodeoxycholic acid sodium
  • 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 Emax 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 .
    KOR agonist 4
  • 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 .
    Ursodeoxycholic acid-13C
  • 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 .
    Mastoparan X
  • HY-P5372
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2

    		Protease Activated Receptor (PAR) Cancer
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2, a bioactive peptide, is a selective Protease activating receptor 1 (PAR-1) agonist over PAR-2. PAR-1 belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. 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' .
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
  • HY-P5372A
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA

    		Protease Activated Receptor (PAR) Cancer
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA, a bioactive peptide, is a selective Protease activating receptor 1 (PAR-1) agonist over PAR-2. PAR-1 belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. 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' .
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 TFA
  • HY-171850
    GLP-1R modulator-1

    		GLP Receptor Metabolic Disease Inflammation/Immunology
    GLP-1R modulator-1 (Compound 384) is an orally active, potent selective glucagon-like peptide-1 receptor (GLP-1R) agonist. GLP-1R modulator-1 activates G-protein coupled signaling, elevates intracellular cAMP levels, promotes insulin secretion, delays gastric emptying and suppresses appetite. GLP-1R modulator-1 is promising for research of type 2 diabetes, obesity, and non-alcoholic steatohepatitis (NASH) .
    GLP-1R modulator-1
  • 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 .
    Ursodeoxycholic acid
  • HY-175197
    MP1202

    		Opioid Receptor Arrestin Neurological Disease
    MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research .
    MP1202
  • HY-N0593
    Deoxycholic acid
    20+ 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 .
    Deoxycholic acid
  • HY-N0593A
    Deoxycholic acid sodium salt
    20+ 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 .
    Deoxycholic acid sodium salt
  • 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 .
    Deoxycholic acid sodium hydrate
  • 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 .
    SBI-810
  • 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 .
    SBI-810 hydrochloride
  • 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 .
    Ursodeoxycholic acid (Standard)
  • 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.
    Guanosine 5'-triphosphate trisodium salt hydrate
  • 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.
    LY2828360
  • 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 .
    Ursodeoxycholic acid-2,2,4,4-d4
  • 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 .
    tBPC
  • HY-N0593S1
    Deoxycholic acid-d5

    		Isotope-Labeled Compounds 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.
    Deoxycholic acid-d5
  • HY-N0593S
    Deoxycholic acid-d4
    1 Publications Verification

    		 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.
    Deoxycholic acid-d4
  • 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.
    Deoxycholic acid-d6
  • HY-N0593R
    Deoxycholic acid (Standard)
    15+ Cited Publications

    Cholanoic Acid(Standard); Desoxycholic acid (Standard)

    		 Reference Standards 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 .
    Deoxycholic acid (Standard)
  • HY-101108R
    Tazarotenic acid (Standard)

    AGN 190299 (Standard)

    		 Reference Standards 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 .
    Tazarotenic acid (Standard)
  • 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.
    Deoxycholic acid-13C
  • HY-N0593AR
    Deoxycholic acid sodium salt (Standard)

    Sodium deoxycholate (Standard)

    		 G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid sodium salt (Standard) is the analytical standard of Deoxycholic acid sodium salt. This product is intended for research and analytical applications. 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 .
    Deoxycholic acid sodium salt (Standard)
  • 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 Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki 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 .
    PCS1055 dihydrochloride
  • 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) .
    Guanosine 5'-diphosphate disodium salt
  • 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 .
    6'-GNTI dihydrochloride
  • HY-P1318
    Ac-RYYRIK-NH2

    		Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=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 .
    Ac-RYYRIK-NH2
  • 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 (Kd=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 .
    Ac-RYYRIK-NH2 TFA
  • 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 .
    Exendin-P5
  • 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 .
    M4 mAChR Modulator-1
  • 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 .
    MRS1067
  • 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 .
    CMF019
  • 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 .
    BPRMU191
  • HY-175556
    CNV-dopamine

    		Dopamine Receptor Neurological Disease
    CNV-dopamine is a photoreleasable D2 receptor-selective agonist. CNV-dopamine activates D2 receptors and induces G protein-coupled inwardly rectifying potassium (GIRK) currents. CNV-dopamine is promising for research of disorders like Parkinson’s disease and addiction .
    CNV-dopamine

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