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Results for "

G-protein coupled receptor 19

" in MCE Product Catalog:

175

Inhibitors & Agonists

5

Screening Libraries

5

Dye Reagents

54

Peptides

5

MCE Kits

18

Natural
Products

34

Recombinant Proteins

15

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • 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.
  • 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.
  • HY-15565
    APD668

    GPR119 Cytochrome P450 Potassium Channel Metabolic Disease
    APD668 is a potent, selective and orally active agonist of G-protein coupled receptor GPR119, with EC50s of 2.7 nM and 33 nM for hGPR119 and rGPR119, respectively. APD668 shows no significant inhibition of any of the five major CYP isoforms with the exception of CYP2C9 (Ki=0.1 μM). APD668 can be used for the research of steatohepatitis and diabetes.
  • HY-B0412
    Estriol

    Oestriol

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-133021
    Arazine

    N-Acetyl-S-farnesyl-L-cysteine

    Others Inflammation/Immunology
    Arazine (N-Acetyl-S-farnesyl-L-cysteine) is a cell-permeable modulator of G protein and G-protein coupled receptor signaling. Arazine can be a a substrate for isoprenylcysteine methyltransferase by competing with prenylated G protein or its receptors site.
  • HY-P0216
    A 779

    Angiotensin Receptor Cardiovascular Disease Endocrinology
    A 779 is a specific antagonist of G-protein coupled receptor (Mas receptor), which is an Ang1-7 receptor distinct from the classical AngII.
  • HY-145562
    Deucrictibant

    Bradykinin Receptor Others
    Deucrictibant is a potent bradykinin receptor antagonist. Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domained family.
  • HY-B0412S1
    Estriol-d1

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d1 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-B0412S
    Estriol-d2

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d2 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-B0412S2
    Estriol-d3

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-d3 is the deuterium labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-114146
    CID 1375606

    Others Metabolic Disease Neurological Disease
    CID 1375606 is a surrogate agonist of orphan G protein-coupled receptor GPR27.
  • HY-W036034A
    GRK-IN-1

    Others Cardiovascular Disease
    GRK-IN-1 is a potential G protein-coupled receptor kinase (GRK) inhibitor.
  • HY-110173
    TC-G 1005

    GPCR19 Metabolic Disease
    TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
  • HY-15291
    MBX-2982

    GPR119 Metabolic Disease
    MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist.
  • HY-123837
    MLS1082

    Dopamine Receptor Neurological Disease
    MLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling.
  • HY-B0412S3
    Estriol-13C3

    Oestriol-13C3

    Estrogen Receptor/ERR Endogenous Metabolite Cancer
    Estriol-13C3 (Oestriol-13C3) is the 13C-labeled Estriol. Estriol is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.
  • HY-114165
    DJ-V-159

    Androgen Receptor Metabolic Disease
    DJ-V-159 is an agonist for G protein-coupled receptor family C group 6 member A (GPRC6A).
  • HY-141495
    PW0464

    Dopamine Receptor Neurological Disease
    PW0464, a nanomolar potent complete G protein biased ligand, is a noncatechol D1R agonist, with an EC50 of 5.8 nM (Gs-cAMP).
  • HY-N0593
    Deoxycholic acid

    Cholanoic Acid; Desoxycholic acid

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-N0593A
    Deoxycholic acid sodium salt

    Sodium deoxycholate

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid sodium salt is specifically responsible for activating the G protein-coupled bile acid receptor TGR5 that stimulates brown adipose tissue (BAT) thermogenic activity.
  • HY-101777
    TC-O 9311

    GPR139 Neurological Disease
    TC-O 9311 is a potent orphan G protein-coupled receptor 139 (GPR139) agonist with an EC50 of 39 nM.
  • HY-109163
    Treprostinil palmitil

    INS-1009

    Prostaglandin Receptor Endocrinology Inflammation/Immunology
    Treprostinil palmitil (TP) is the prodrug of DP1 and EP2 agonist, Treprostinil (UT-15), whose EC50 values were 0.6 and 6.2 nM, respectively. Treprostinil palmitil is a pure prodrug and possesses no inherent binding to G-protein coupled receptors including prostanoid receptors.
  • HY-103449
    G15

    Estrogen Receptor/ERR Cancer
    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  • HY-10499
    PH-064

    BIM-46187

    Others Neurological Disease
    PH-064 (BIM-46187) is an inhibitor of heterotrimeric G-protein complex.
  • HY-70075
    CCG-63808

    RGS Protein Cancer
    CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
  • HY-124622
    NNC-0640

    Glucagon Receptor Metabolic Disease
    NNC-0640 is a potent human G-protein-coupled glucagon receptor (GCGR) negative allosteric modulator (NAM) with an IC50 of 69.2 nM.
  • HY-P1306
    Obestatin(rat)

    GHSR Inflammation/Immunology Cardiovascular Disease
    Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
  • HY-135542
    NBI-27914

    CRFR Others
    NBI-27914 is a potent and selective antagonist of CRFR1. The CRF receptors, CRFR1 and CRFR2, are members of the G protein-coupled receptor superfamily.
  • HY-P0195
    Bombesin

    Bombesin Receptor Metabolic Disease Neurological Disease
    Bombesin, a tetradecapeptide, plays an important role in the release of gastrin and the activation of G-protein receptors.
  • HY-134801
    CID1231538

    Others Metabolic Disease Inflammation/Immunology
    CID1231538, a benzothiazole analogue, is a potent GPR35 antagonist (IC50=0.55 μM). GPR35 is a G protein-coupled receptor (GPCR).
  • HY-138686
    GPR30 agonist-1

    Estrogen Receptor/ERR Endocrinology Cardiovascular Disease
    GPR30 agonist-1 is a G protein-coupled receptor 30 (GPR30) agonist. GPR30 agonist-1 exerts vasorelaxant effects.
  • HY-110285
    ML382

    Others Neurological Disease
    ML382 is a potent and selective MRGPRX1 (Mas-related G protein-coupled receptor X1, MrgX1) positive allosteric modulator, with an EC50 of 190 nM.
  • HY-P1306A
    Obestatin(rat) TFA

    GHSR Inflammation/Immunology Cardiovascular Disease
    Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
  • HY-103080
    CMF019

    Others Cardiovascular Disease
    CMF019 is a 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.
  • HY-19863
    F-15599

    NLX-101

    5-HT Receptor Neurological Disease
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
  • HY-N0593S1
    Deoxycholic acid-d5

    GPCR19 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

    GPCR19 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-130118
    MRGPRX1 agonist 1

    Others Neurological Disease
    MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect.
  • HY-P1438
    Neuropeptide S(Rat)

    Neuropeptide Y Receptor Neurological Disease
    Neuropeptide S (Rat) is an endogenous ligand of a previously orphan G-protein-coupled receptor now named NPS receptor. Neuropeptide S (Rat) can be used for the research of nervous system disease.
  • HY-P3108
    Alamandine

    Angiotensin Receptor Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Alamandine, a member of the renin-angiotensin system (RAS), a vasoactive peptide, is an endogenous ligand of the G protein-coupled receptor MrgD. Alamandine targets to protect the kidney and heart through anti-hypertensive actions.
  • HY-10957
    L-692429

    MK-0751

    GHSR Metabolic Disease
    L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.
  • HY-P1483
    Urotensin II, mouse

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse is a potent vasoconstrictor. Urotensin II, mouse plays a physiological role in the central nervous system.
  • HY-134661
    (S)-CVN424

    Others Neurological Disease
    (S)-CVN424 is a potent G-Protein-Coupled Receptor 6 (GPR6) modulator. (S)-CVN424 has the potential for a variety of neurological and psychiatric disorders research, including Parkinson's disease.
  • HY-P1483B
    Urotensin II, mouse acetate

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse acetate is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse acetate is a potent vasoconstrictor. Urotensin II, mouse acetate plays a physiological role in the central nervous system.
  • HY-13771A
    Ursodeoxycholic acid sodium

    Ursodeoxycholate sodium; Ursodiol sodium; UCDA sodium

    GPCR19 FXR Endogenous Metabolite Cancer Metabolic Disease Inflammation/Immunology
    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

    Ursodeoxycholate; Ursodiol; UDCA

    GPCR19 FXR Endogenous Metabolite 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. Orally active.
  • HY-101033
    GPR35 agonist 1

    Others Cancer Endocrinology
    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
  • HY-135303
    GLPG1205

    GPR84 Inflammation/Immunology
    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
  • HY-N0593S2
    Deoxycholic acid-d6

    Cholanoic Acid-d6; Desoxycholic acid-d6

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid-d6 (Cholanoic 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-119222
    GSK256073

    GPR109A Metabolic Disease
    GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
  • HY-P1483A
    Urotensin II, mouse TFA

    Urotensin Receptor Neurological Disease Cardiovascular Disease
    Urotensin II, mouse TFA is an endogenous ligand for the orphan G-protein-coupled receptor GPR14 or SENR. Urotensin II, mouse TFA is a potent vasoconstrictor. Urotensin II, mouse TFA plays a physiological role in the central nervous system.
  • HY-108699
    TM-N1324

    GHSR Neurological Disease Endocrinology
    TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn 2+, and 280 nM/180 nM in the absence of Zn 2+ for human/murine GPR39.
  • HY-18991
    CCG215022

    PKA Cancer
    CCG215022 is a G protein-coupled receptor kinases (GRKs) inhibitor with IC50s of 0.15±0.07 μM, 0.38±0.06 μM and 3.9±1 μM for GRK2, GRK5 and GRK1, respectively.
  • HY-18990
    GSK180736A

    ROCK Cardiovascular Disease
    GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  • HY-112779
    Pertussis Toxin

    Others Infection
    Pertussis Toxin is a protein-based AB5-type exotoxin produced by the bacterium Bordetella pertussis, which causes whooping cough. Pertussis Toxin inhibits G protein-coupled receptor (GPR) signaling through Gi proteins.
  • HY-101483
    Dihydromunduletone

    DHM

    Others Cancer Neurological Disease
    Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.
  • HY-N0593S3
    Deoxycholic acid-13C

    Cholanoic Acid-13C; Desoxycholic acid-13C

    GPCR19 Endogenous Metabolite Metabolic Disease
    Deoxycholic acid-13C (Cholanoic 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-126855
    Cholic acid 7-sulfate

    7-Sulfocholic acid

    GPCR19 Metabolic Disease
    Cholic acid 7-sulfate (7-Sulfocholic acid), a metabolite of Cholic acid, is a Takeda G-protein receptor 5 (TGR5) agonist. Cholic acid 7-sulfate can increase Tgr5 expression and induce GLP-1 secretion.
  • HY-13771S
    Ursodeoxycholic acid-d5

    Ursodiol-d5; UDCA-d5

    GPCR19 FXR Endogenous Metabolite Metabolic Disease Cancer
    Ursodeoxycholic acid-d5 (Ursodiol-d5) is the deuterium labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
  • HY-138193
    Lauryl maltose neopentyl glycol

    LMNG

    Others Others
    Lauryl maltose neopentyl glycol (LMNG) is a detergent that can solubilize and stabilize membrane proteins. Lauryl maltose neopentyl glycol extracts integral membrane proteins from membranes, and improves substantially the stability of various membrane proteins, including G protein-coupled receptors and respiratory complexes.
  • HY-136561
    GRK5-IN-2

    Others Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
  • HY-115768
    Compound 48/80

    Poly-p-methoxyphenethylmethylamine

    Others Cancer Neurological Disease
    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-50162
    GPR120 modulator 1

    GPR120 Metabolic Disease
    GPR120 modulator 1 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F1. GPR120 modulator 1 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-50172
    GPR120 modulator 2

    GPR120 Metabolic Disease
    GPR120 modulator 2 is a G protein coupled receptor 120 (GPR120) modulator extracted from patent US8394841B2, compound example F13. GPR120 modulator 2 can be used for the research of diseases associated with abnormal or deregulated GPR120, such as diabetes.
  • HY-B1811
    Vasopressin

    Endogenous Metabolite Neurological Disease
    Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.
  • HY-142817
    GRK6-IN-2

    Others Cancer
    GRK6-IN-2 (compound 10a) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-2 has the potential for the research of multiple myeloma.
  • 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 Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.
  • HY-110098
    Ro 5212773

    EPPTB

    Others 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.
  • HY-134494
    MS48107

    Others Neurological Disease
    MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice.
  • HY-108020
    LY2881835

    GPR40 Endocrinology
    LY2881835 is a potent and selective agonist of G protein-coupled receptor 40 (GPR40). LY2881835 has efficacious and durable dose-dependent reductions in glucose levels along with significant increases in insulin and GLP-1 secretion. LY2881835 has the potential for the research of type 2 diabetes mellitus.
  • HY-142812
    GRK6-IN-1

    Others Cancer
    GRK6-IN-1 (compound 18) is a potent inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 of 120 nM. GRK6 is a critical kinase required for the survival of multiple myeloma (MM) cells. GRK6-IN-1 has the potential for the research of multiple myeloma.
  • HY-120006A
    (rel)-AR234960

    ERK Cardiovascular Disease
    (rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  • HY-B1816
    Zaprinast

    M&B 22948

    Phosphodiesterase (PDE) Neurological Disease Cardiovascular Disease Endocrinology
    Zaprinast (M&B 22948) is an inhibitor of cGMP-selective Phosphodiesterases(PDEs). Zaprinast is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately. Zaprinast reduces vessel remodeling through antiproliferative and proapoptotic effects.
  • HY-P1525
    Melanin Concentrating Hormone, salmon

    MCH (salmon)

    MCHR1 (GPR24) Metabolic Disease Neurological Disease Cardiovascular Disease Endocrinology
    Melanin Concentrating Hormone, salmon is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
  • HY-B0228
    Adenosine

    Adenine riboside; D-Adenosine

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Endogenous Metabolite Cancer Metabolic Disease
    Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
  • HY-117779
    DBIBB

    Apoptosis Endocrinology
    DBIBB is a specific nonlipid agonist of the type 2 G protein coupled receptor for lysophosphatidic acid (LPA2). DBIBB mitigates the gastrointestinal radiation syndrome, increases intestinal crypt survival and enterocyte proliferation, and reduces apoptosis. DBIBB represents a drug candidate capable of mitigating acute radiation syndrome caused by high-dose γ-radiation to the hematopoietic and gastrointestinal system.
  • HY-P1525A
    Melanin Concentrating Hormone, salmon TFA

    MCH (salmon) (TFA)

    MCHR1 (GPR24) Metabolic Disease Neurological Disease Cardiovascular Disease Endocrinology
    Melanin Concentrating Hormone, salmon TFA (MCH (salmon) TFA) is a 19-amino-acid neuropeptide initially identified in the pituitary gland of teleost fish, which regulates food intake, energy balance, sleep state, and the cardiovascular system. Melanin-concentrating hormone is a ligand for an orphan G protein-coupled receptor (SLC-1/GPR24) and MCHR2.
  • HY-103450
    G36

    Estrogen Receptor/ERR Endocrinology
    G-36 is a cell permeable non-steroidal antagonist of G-protein-coupled estrogen receptor (GPER/GPR30) which selectively inhibits estrogen-mediated activation of PI3K by GPER, but not by ERα. G-36 also inhibits estrogen-mediated calcium mobilization (IC50=112 nM).
  • HY-12649
    Y16

    Ras Cancer
    Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP.
  • HY-109562A
    CCG258208 hydrochloride

    GRK2-IN-1 hydrochloride

    Others Cardiovascular Disease
    GRKs-IN-1 hydrochloride, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=130 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 hydrochloride is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-109562
    CCG258208

    GRKs-IN-1

    Others Cardiovascular Disease
    GRKs-IN-1, Compound 14as, has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50=30 nM) and GRK5 (IC50=7.1 μM). GRKs-IN-1 is a derivative 14as of paroxetine, shows a 100-fold improvement in cardiomyocyte contractility assays over paroxetine.
  • HY-W014502
    D-Kynurenine

    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).
  • 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.
  • HY-12695B
    Guanosine 5'-triphosphate trisodium salt hydrate

    5'-GTP trisodium salt hydrate

    Others Endogenous Metabolite 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-14899
    Taprenepag

    CP-544326

    Prostaglandin Receptor Endocrinology
    Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors.
  • HY-139690
    CCG258747

    Opioid Receptor Cardiovascular Disease
    CCG258747 is a selective GRK2 inhibitor (IC50=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.
  • HY-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.
  • 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-106224
    Orexin A (human, rat, mouse)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. 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-13509
    CCG-50014

    RGS Protein Inflammation/Immunology
    CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site. CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test.
  • HY-121532
    (-)-Rasfonin

    Ras Apoptosis Autophagy Cancer
    (-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line).
  • HY-U00431
    CCG 203769

    RGS Protein Neurological Disease
    CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
  • HY-139677
    5-HT7R antagonist 1

    GPCR19 Neurological Disease
    5-HT7R antagonist 1 is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
  • HY-B0228S
    Adenosine-d1

    Adenine riboside-d1; D-Adenosine-d1

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Endogenous Metabolite Cancer Metabolic Disease
    Adenosine-d1 (Adenine riboside-d1) is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
  • HY-19835
    LY2922470

    GPR40 Metabolic Disease
    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
  • HY-128121
    MLS1547

    Dopamine Receptor Neurological Disease
    MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM).
  • HY-106224A
    Orexin A (human, rat, mouse) (TFA)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. 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.
  • HY-P1349A
    Orexin B, rat, mouse TFA

    Rat orexin B TFA; Orexin B (mouse) (TFA)

    Orexin Receptor (OX Receptor) Endocrinology Neurological Disease
    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-143864
    S1PR1 agonist 1

    LPL Receptor Inflammation/Immunology
    S1PR1 agonist 1 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 1 has the potential for the research of autoimmune diseases (extracted from patent WO2021175223A1, compound 22).
  • HY-143865
    S1PR1 agonist 2

    LPL Receptor Inflammation/Immunology
    S1PR1 agonist 2 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 2 has the potential for the research of autoimmune diseases (extracted from patent WO2021175225A1, compound 1).
  • HY-139677A
    5-HT7R antagonist 1 free base

    GPCR19 Neurological Disease
    5-HT7R antagonist 1 (free base) is a G protein-biased antagonist against 5-HT7R (Ki = 6.5 nM).
  • HY-12695
    Guanosine 5'-triphosphate trisodium salt

    5'-GTP trisodium salt

    Endogenous Metabolite Others
    Guanosine 5'-triphosphate trisodium salt (5'-GTP trisodium salt) is an activator of the signal transducing G proteins which are involved in various cellular processes including proliferation, differentiation, and activation of several intracellular kinase cascades.
  • HY-12700
    RO5256390

    Others Neurological Disease
    RO5256390 is an agonist of trace amine-associated receptor 1 (TAAR1), a highly conserved G-protein-coupled receptor (GPCR) bound by endogenous trace amines. RO5256390 can be used to reduce multiple behavioral effects of drugs of abuse through their actions on the mesocorticolimbic system. RO5256390 is a modulator of monoaminergic neurotransmission, blocks psychostimulant-induced hyperactivity and produces a brain activation pattern reminiscent of the antipsychotic drug olanzapine, suggesting antipsychotic-like properties.
  • HY-108496
    Sphingosine-1-phosphate

    S1P

    Endogenous Metabolite LPL Receptor Endocrinology
    Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
  • HY-108635
    C16-PAF

    PAF (C16)

    p38 MAPK MEK ERK Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    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-P1066
    Apelin-17(human, bovine)

    HIV Infection
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-P1065
    Apelin-36(rat, mouse)

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-W010737
    Guanosine-5'-triphosphate disodium salt

    5'-GTP disodium salt

    Endogenous Metabolite Metabolic Disease
    Guanosine-5'-triphosphate disodium salt (5'-GTP trisodium salt) 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-133735A
    GRP-60367 hydrochloride

    Others Infection
    GRP-60367 hydrochloride is a first-in-class small-molecule rabies virus (RABV) entry inhibitor with nanomolar potency against some RABV strains. GRP-60367 hydrochloride specifically targets the RABV G protein.
  • HY-15589
    GW9508

    GPR40 Potassium Channel Metabolic Disease Inflammation/Immunology Cardiovascular Disease
    GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
  • HY-P1065A
    Apelin-36(rat, mouse) TFA

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ.
  • HY-P1066A
    Apelin-17(human, bovine) TFA

    HIV Infection
    Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-108601A
    Ro 32-0432 hydrochloride

    PKC Inflammation/Immunology Neurological Disease
    Ro 32-0432 hydrochloride is a potent, selective, ATP-competitive and orally active PKC inhibitor. The IC50 values of Ro 32-0432 hydrochloride for PKCα, PKCβI, PKCβII, PKCγ and PKCε are 9.3 nM, 28 nM, 30 nM, 36.5 nM and 108.3 nM, respectively. Ro 32-0432 hydrochloride is also a selective G protein-coupled receptor kinase 5 (GRK5) inhibitor. Ro 32-0432 hydrochloride prevents T-cell activation and has the potential for chronic inflammatory and autoimmune diseases research.
  • HY-P1345
    TLQP-21

    Complement System Endocrinology Neurological Disease
    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-P1345A
    TLQP-21 TFA

    Complement System Endocrinology Neurological Disease
    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-D0254
    Gallein

    Pyrogallol phthalein

    Others Cancer
    Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent. Gallein used as a red dye, an acid-base indicator and as a detection reagent for phosphates.
  • HY-P2141
    TRV-120027

    Angiotensin Receptor Cardiovascular Disease
    TRV120027, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 has the potential for the acute decompensated heart failure (ADHF) treatment.
  • HY-P2141A
    TRV-120027 TFA

    Angiotensin Receptor Cardiovascular Disease
    TRV120027 TFA, a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R), engages ß-arrestins while blocking G-protein signaling. TRV120027 TFA induces acute catecholamine secretion through cation channel subfamily C3 (TRPC3) coupling, promotes the formation of a macromolecular complex composed of AT1R–β-arrestin-1–TRPC3–PLCγ at the plasma membrane. TRV120027 TFA inhibits angiotensin II–mediated vasoconstriction and increases cardiomyocyte contractility. TRV120027 TFA has the potential for the acute decompensated heart failure (ADHF) treatment.
  • 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-12745A
    Nalfurafine hydrochloride

    TRK-820 hydrochloride

    Opioid Receptor Neurological Disease
    Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-12745
    Nalfurafine

    TRK-820

    Opioid Receptor Neurological Disease
    Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
  • HY-P1064
    Apelin-36(human)

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-14563
    VU10010

    mAChR Neurological Disease
    VU10010 is a potent, highly selective and allosteric M4 mAChR potentiator with an EC50 of 400 nM. VU10010 binds to an allosteric site on M4 mAChR and increases affinity for acetylcholine and coupling to G proteins. VU10010 increases carbachol-induced depression of transmission at excitatory but not inhibitory synapses in the hippocampus.
  • HY-108496S
    Sphingosine-1-phosphate-d7

    S1P-d7

    Endogenous Metabolite LPL Receptor Endocrinology
    Sphingosine-1-phosphate-d7 (S1P-d7) is the deuterium labeled Sphingosine-1-phosphate. Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca 2+ as an extracellular ligand for G protein-coupled receptors. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids.
  • HY-P1064A
    Apelin-36(human) TFA

    HIV Infection Metabolic Disease Cardiovascular Disease
    Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-108400
    SCH-23390 maleate

    R-(+)-SCH-23390 maleate

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-19545A
    SCH-23390 hydrochloride

    R-(+)-SCH-23390 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-120645
    BMS-986122

    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.
  • HY-111557
    YM-254890

    P2Y Receptor Cardiovascular Disease
    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.
  • HY-112705
    VU0529331

    Potassium Channel Neurological Disease
    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-144655
    IP2

    Others Cancer
    IP2 is an immunomodulatory agent. IP2 increases PTP (Pioneer Translation Product)-derived antigen presentation in cancer cells. IP2 shows non-cytotoxic for cancer cells. IP2 induces tumor growth defects in mouse.
  • HY-13948
    Angiotensin II human

    Angiotensin II; Ang II; DRVYIHPF

    Angiotensin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Angiotensin II (Angiotensin II) is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis. Angiotensin II induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-19545AS
    SCH-23390-d3 hydrochloride

    Dopamine Receptor 5-HT Receptor Potassium Channel Neurological Disease
    SCH-23390-d3 (R-(+)-SCH-23390-d3) hydrochloride is the deuterium labeled SCH-23390 hydrochloride. SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-115831
    SAR247799

    S1P1 agonist 3

    LPL Receptor Cardiovascular Disease
    SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.
  • HY-107146
    PZ-128

    P1pal-7

    Protease-Activated Receptor (PAR) Cancer Cardiovascular Disease
    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-P0172A
    ATI-2341 TFA

    CXCR Cancer Inflammation/Immunology Endocrinology
    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-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-117163
    FzM1.8

    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 binding stabilizes FZD4 with an increased affinity for heterotrimeric G protein and stimulates the release of the Gβγ subunit that in turn activates PI3K.
  • HY-13948B
    Angiotensin II human TFA

    Angiotensin II TFA; Ang II TFA; DRVYIHPF TFA

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human (Angiotensin II) TFA is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human TFA plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human TFA stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human TFA induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human TFA also induces apoptosis. Angiotensin II human TFA induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-13948A
    Angiotensin II human acetate

    Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate

    Angiotensin Receptor Apoptosis Cancer Endocrinology Cardiovascular Disease
    Angiotensin II human (Angiotensin II) acetate is a vasoconstrictor and a major bioactive peptide of the renin/angiotensin system. Angiotensin II human acetate plays a central role in regulating human blood pressure, which is mainly mediated by interactions between Angiotensin II and the G-protein-coupled receptors (GPCRs) Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis. Angiotensin II human acetate induces capillary formation from endothelial cells via the LOX-1 dependent redox-sensitive pathway.
  • HY-112461A
    NF449 octasodium

    P2X Receptor Cardiovascular Disease
    NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a G-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
  • HY-103411
    SKF83822 hydrobromide

    Dopamine Receptor Neurological Disease
    SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors.
  • HY-N2464
    Maltotetraose

    Amylotetraose; Fujioligo 450; α-1,4-Tetraglucose

    Endogenous Metabolite Metabolic Disease
    Maltotetraose can be used as a substrate for the enzyme-coupled determination of amylase activity in biological fluids.
  • HY-102076
    0990CL

    Others Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
  • HY-B0445
    NAD+

    β-DPN; β-NAD; β-Nicotinamide Adenine Dinucleotide

    Endogenous Metabolite Metabolic Disease
    NAD+ is a coenzyme composed of ribosylnicotinamide 5'-diphosphate coupled to adenosine 5'-phosphate by pyrophosphate linkage.
  • HY-42360
    SMCC

    ADC Linkers Cancer
    SMCC is a protein crosslinker. SMCC-conjugated antigen coupled spleen cells to induce antigen-specific immune responses.
  • HY-135717
    Norbiotinamine

    Others Cancer
    Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
  • HY-135717A
    Norbiotinamine hydrochloride

    Others Cancer
    Norbiotinamine hydrochloride is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
  • HY-101202
    SNC80

    NIH 10815

    Opioid Receptor Neurological Disease
    SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
  • HY-122203
    PCS1055 dihydrochloride

    mAChR AChE 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.
  • HY-B1477
    Clopamide

    Sodium Channel Metabolic Disease Cardiovascular Disease
    Clopamide is an orally active thiazide-like diuretic agent that inhibits the sodium-coupled chloride cotransporter SLC12A3. Clopamide has the potential for hypertension and cardiac failure research.
  • HY-W041994
    GMBS

    Others Cancer
    GMBS is a heterobifunctional cross-linker. GMBS can be used in chemical cross-linking of proteins coupled with mass spectrometry (CXMS) to study protein folding and to map the interfaces between interacting proteins.
  • HY-111763
    GPR40/FFAR1 modulator 1

    GPR40 Metabolic Disease
    GPR40/FFAR1 modulator 1 is an agonist and an allosteric modulator for Gq-coupled free fatty acid receptor 1 (GPR40/FFAR1).
  • HY-N2368A
    Arecaidine hydrochloride

    GABA Receptor Neurological Disease
    Arecaidine hydrochloride, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine hydrochloride is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
  • HY-N2368
    Arecaidine

    GABA Receptor Neurological Disease
    Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
  • HY-112197
    PKG drug G1

    Others Cardiovascular Disease
    PKG drug G1 targets C42 of PKG Iα. PKG drug G1 can couple to vasodilation and blood pressure lowering by a C42 PKG Iα-independent mechanism.
  • HY-101884A
    Biotinylated-D-lysine TFA

    Others Neurological Disease
    Biotinylated-D-lysine TFA is a conjugate of L-biotin and D-lysine, where the carboxylate of L-biotin is coupled with the ϵ-amine of D-lysine via a secondary amide bond. Biotinylated-D-lysine TFA is an isomer of the neuroanatomical tracer Biocyte.
  • HY-B1477S
    Clopamide-d6

    Sodium Channel Metabolic Disease Cardiovascular Disease
    Clopamide-d6 is the deuterium labeled Clopamide. Clopamide is an orally active thiazide-like diuretic agent that inhibits the sodium-coupled chloride cotransporter SLC12A3. Clopamide has the potential for hypertension and cardiac failure research.
  • HY-B1700A
    Mivacurium dichloride

    nAChR Neurological Disease
    Mivacurium dichloride is a benzylisoquinoline derivative and is a short-acting non-depolarizing neuromuscular blocking agent and skeletal muscle relaxant. Mivacurium dichloride couples with the nAChR to reduce or inhibit the depolarizing effect of acetylcholine on the terminal disc of the muscle cell.
  • HY-131768
    2'-O-Succinyl-cAMP

    Others Others
    2'-O-Succinyl-cAMP is a cAMP analog that can be covalently coupled to acetylcholinesterase. 2'-O-Succinyl-cAMP conjugate has been used as tracers in a classical heterogeneous competitive enzyme immunoassay allowing the determination of cAMP.
  • HY-N7330
    Integracin B

    HIV Integrase HIV Infection
    Integracin B is a potent dimeric alkyl aromatic inhibitor of HIV-1 integrase discovered from the screening of fungal extracts using an in vitro assay. Integracin B inhibits both coupled and strand transfer activity of HIV-1 integrase.
  • HY-110202
    MRS5698

    Adenosine Receptor Inflammation/Immunology Neurological Disease
    MRS5698 is a selective Gi protein-coupled A3 adenosine receptor (A3AR) agonist, with Kis of approximately 3 nM for human and mouse A3AR, respectively. MRS5698 can be used for the research of pain and psoriasis.
  • HY-103320A
    Calhex 231 hydrochloride

    CaSR Metabolic Disease
    Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • HY-115747
    Namoline

    Histone Demethylase Cancer
    Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research.
  • HY-133018
    HCV-IN-7

    HCV Infection
    HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
  • HY-133018A
    HCV-IN-7 hydrochloride

    HCV Cancer
    HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 hydrochloride shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 hydrochloride has anti-viral activity.
  • HY-101884
    Biocytin

    (+)-Biocytin

    Endogenous Metabolite Neurological Disease
    Biocytin is a conjugate of D-biotin and L-lysine, where the carboxylate of D-biotin is coupled with the ϵ-amine of L-lysine via a secondary amide bond. Biocytin is a classical neuroanatomical tracer commonly used to map brain connectivity. Biocytin is used as a versatile marker in anterograde, retrograde and intracellular neuroanatomical investigations and in biotinidase assays.
  • HY-19625
    MCB-613

    Others Cancer
    MCB-613 is a potent Steroid receptor coactivator SRC small molecule ‘stimulator’ (SMS), super-stimulates SRCs’ transcriptional activity. MCB-613 increases SRCs’ interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 is a SMS that target oncogenes can be exploited as anti-cancer agents by over-stimulating the SRC oncogenic program.
  • HY-124825
    iGOT1-01

    Others Cancer
    iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC50s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity.
  • HY-113439
    12-HETE

    Apoptosis Inflammation/Immunology Cardiovascular Disease
    12-HETE, a major metabolic product of arachidonic acid using 12-LOX catalysis, inhibits cell apoptosis in a dose-dependent manner. 12-HETE promotes the activation and nuclear translocation of NF-κB through the integrin-linked kinase (ILK) pathway.12-HETE has both anti-thrombotic and pro-thrombotic effects. 12-HETE is a neuromodulator.
  • HY-P1111
    Lyn peptide inhibitor

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-P1111A
    Lyn peptide inhibitor TFA

    Src Interleukin Related Inflammation/Immunology
    Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of  asthma, allergic, and other eosinophilic disorders.
  • HY-103211
    L748337

    Adrenergic Receptor Cancer Metabolic Disease Cardiovascular Disease
    L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively. L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6. L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases.
  • HY-134807
    Indophagolin

    P2X Receptor 5-HT Receptor Autophagy Cancer
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.