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G-protein Activator

" in MedChemExpress (MCE) Product Catalog:

144

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4

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1

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43

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3

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10

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13771
    Ursodeoxycholic acid
    25+ Cited Publications

    Ursodeoxycholate; Ursodiol; UDCA

    G protein-coupled Bile Acid Receptor 1 FXR Angiotensin-converting Enzyme (ACE) Endogenous Metabolite Infection Metabolic Disease Cancer
    Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active .
    Ursodeoxycholic acid
  • HY-N0593
    Deoxycholic acid
    25+ 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-115768
    Compound 48/80
    5 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-N0593A
    Deoxycholic acid sodium salt
    Maximum Cited Publications
    27 Publications Verification

    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-W010737

    5'-GTP disodium salt

    Exosomes Endogenous Metabolite MicroRNA Metabolic Disease
    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 .
    Guanosine-5'-triphosphate disodium salt
  • HY-113066A
    Guanosine 5'-diphosphate disodium salt
    2 Publications Verification

    GDP disodium salt

    Hepcidin Potassium Channel Endogenous Metabolite Neurological Disease Inflammation/Immunology Cancer
    Guanosine 5'-diphosphate (GDP) disodium salt, a purine nucleoside diphosphate, is interconverted to guanosine by the action of exonucleotidase and phosphorylation of nucleoside to guanine. Guanosine 5'-diphosphate disodium salt activates adenosine 5'-triphosphate-sensitive K + channel and is used to study the kinetics and characteristics of GTPases such as those associated with G-protein coupled receptors (GPCR). Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the Hepcidin (HY-P70400)-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Elevated levels of guanosine 5’-diphosphate are associated with the pathogenesis of neurological diseases. Guanosine 5'-diphosphate disodium salt is promising for the research of inflammation, such as anemia of inflammation (AI) .
    Guanosine 5'-diphosphate disodium salt
  • HY-108635
    C16-PAF
    Maximum Cited Publications
    40 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 .
    C16-PAF
  • HY-12695
    Guanosine 5'-triphosphate trisodium
    5 Publications Verification

    5'-GTP trisodium

    Exosomes Endogenous Metabolite DNA/RNA Synthesis Metabolic Disease
    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 trisodium salt holds promise for research in biosynthesis and skeletal muscle regeneration .
    Guanosine 5'-triphosphate trisodium
  • HY-137677B

    Guanosine 5'-[γ-thio]triphosphate tetralithium

    GLUT Metabolic Disease
    GTPγS (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-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-B1816
    Zaprinast
    3 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 .
    Zaprinast
  • HY-W014502

    Aryl Hydrocarbon Receptor Endogenous Metabolite Cancer
    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) .
    D-Kynurenine
  • 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-P99394
    Talquetamab
    1 Publications Verification

    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 .
    Talquetamab
  • 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-13771A
    Ursodeoxycholic acid sodium
    25+ Cited Publications

    Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium

    G protein-coupled Bile Acid Receptor 1 FXR Endogenous Metabolite Metabolic Disease Inflammation/Immunology Cancer
    Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active .
    Ursodeoxycholic acid sodium
  • 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-P0172
    ATI-2341
    4 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) .
    ATI-2341
  • HY-103450

    Estrogen Receptor/ERR Endocrinology Cancer
    G-36 is a cell-permeable nonsteroidal antagonist of the G protein-coupled estrogen receptor (GPER/GPR30), which selectively inhibits estrogen-mediated PI3K activation through GPER, rather than Erα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM). G-36 is promising for research in the field of cancer .
    G36
  • 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-137167

    Gpp(NH)p lithium

    Adenylate Cyclase Metabolic Disease
    Guanylyl imidodiphosphate lithium (Gpp (NH) p lithium) is a non-hydrolyzable GTP analog. Guanylyl imidodiphosphate lithium increases adenylate cyclase activity. Guanylyl imidodiphosphate lithium binds to and irreversibly activates G proteins .
    Guanylyl imidodiphosphate lithium
  • HY-110098
    Ro 5212773
    1 Publications Verification

    EPPTB

    Trace Amine-associated Receptor (TAAR) Neurological Disease
    Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids .
    Ro 5212773
  • HY-P1241
    BAM(8-22)
    1 Publications Verification

    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 .
    BAM(8-22)
  • HY-113478S

    Ursodeoxycholate-d4; Ursodiol-d4; UDCA-d4

    Isotope-Labeled Compounds Infection Metabolic Disease
    Ursodeoxycholic acid-2,2,4,4-d4 is the deuterium labeled Ursodeoxycholic acid (HY-13771). Ursodeoxycholic acid is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection .
    Ursodeoxycholic acid-d4
  • HY-12695B

    5'-GTP trisodium salt hydrate

    Exosomes Endogenous Metabolite DNA/RNA Synthesis Metabolic Disease
    Guanosine 5'-triphosphate (5'-GTP) trisodium salt hydrate 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 hydrate 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 hydrate holds promise for research in biosynthesis and skeletal muscle regeneration .
    Guanosine 5'-triphosphate trisodium salt hydrate
  • HY-120645
    BMS-986122
    1 Publications Verification

    Opioid Receptor Neurological Disease
    BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
    BMS-986122
  • HY-16642A
    LY2828360
    1 Publications Verification

    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-103080

    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-107541
    O-1602
    1 Publications Verification

    GPR55 Neurological Disease
    O-1602 is an agonist of GPR55 (G protein-coupled receptor 55). O-1602 reduces the number and activation of hippocampal microglia induced by METH (methamphetamine). O-1602 decreases the expression levels of NLRP3 inflammasome proteins, including NLRP3, ASC and Caspase-1 .
    O-1602
  • HY-P0172A
    ATI-2341 TFA
    4 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) .
    ATI-2341 TFA
  • HY-120967

    p38 MAPK Akt Interleukin Related Cancer
    (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98%, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT (triethylamine), in ethanol:chloroform (1:1), 98% can be used for the research of ovarian cancer .
    (2S)-OMPT triethylamine, in ethanol:chloroform (1:1), 98%
  • HY-130345

    Platelet-activating Factor Receptor (PAFR) Cardiovascular Disease
    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 .
    PAF (C18)
  • HY-117163
    FzM1.8
    1 Publications Verification

    Wnt β-catenin Cancer
    FzM1.8, derives from FzM1, is an allosteric agonist of FZD4 with pEC50 of 6.4. FzM1.8 binds to FZD4 and activates the WNT/β-catenin pathway, by promoting TCF/LEF transcriptional activity in the absence of any WNT ligand. FzM1.8 stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K .
    FzM1.8
  • HY-19835

    Free Fatty Acid Receptor Metabolic Disease
    LY2922470 is a selective and orally active agonist for the G protein-coupled receptor 40 (GPR40). LY2922470 activates GPR40-mediated β-arrestin recruitment with EC50s of 7 nM (human GPR40), 1 nM (mouse GPR40) and 3 nM (rat GPR40). LY2922470 can be used for research of type 2 diabetes mellitus (T2DM) .
    LY2922470
  • HY-13771R

    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-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-120967A

    p38 MAPK Akt Interleukin Related Cancer
    (2S)-OMPT, Lysophosphatidic acid analogue, is a LPA3 G-protein-coupled receptor agonist. (2S)-OMPT selectively activates LPA3 G-protein-coupled receptor to trigger downstream cellular signaling events. (2S)-OMPT induces calcium, IL-6 release in cancer cells and activates MAPK and Akt signaling pathways. (2S)-OMPT can be used for the research of ovarian cancer .
    (2S)-OMPT
  • HY-P2544

    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 Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively .
    [Lys8, Lys9]-Neurotensin (8-13)
  • HY-P3136

    TRV120055

    Angiotensin Receptor ERK Cardiovascular Disease
    TRV055 (TRV120055) is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV120055 induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. TRV055 activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. TRV055 induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. TRV055 can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses [1]
    TRV055
  • HY-P2705

    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-N0593R
    Deoxycholic acid (Standard)
    20+ 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-N0593AR

    Sodium deoxycholate (Standard)

    G protein-coupled Bile Acid Receptor 1 Endogenous Metabolite Reference Standards 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-P10716

    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-135065

    Trace Amine-associated Receptor (TAAR) Metabolic Disease
    3-Iodothyronamine (hydrochloride) is an endogenous and rapid-acting derivative of thyroid hormone. 3-Iodothyronamine potently activates an orphan G protein-coupled receptor in vitro (TAAR1) and induced hypothermia in vivo on a rapid time scale. 3-Iodothyronamine can be used for the research of congestive heart failure .
    3-Iodothyronamine hydrochloride
  • HY-P3136A

    TRV120055 hydrochloride

    Angiotensin Receptor Cardiovascular Disease
    TRV055 (TRV120055) hydrochloride is a G protein-biased agonist of angiotensin II type 1 receptors (AT1Rs). TRV055 hydrochloride induces fibroblast proliferation, overexpression of collagen I and α-SMA, and stress fibre formation in human cardiac fibroblasts. RV055 hydrochloride activates AT1 receptor/Gαq-mediated signaling pathways, upregulates TGF-β1 and p-ERK1/2. RV055 hydrochloride induces collagen secretion in adult rat myofibroblasts at a level comparable to Ang II. RV055 hydrochloride can be used to study the role of G protein-biased signaling of AT1Rs in regulating fibrotic responses [1]
    TRV055 hydrochloride
  • HY-141581

    Platelet-activating Factor Receptor (PAFR) Endogenous Metabolite Cardiovascular Disease
    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 .
    Lyso-PAF C-18
  • HY-P5372A

    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-115575

    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

    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-N0593S3

    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

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