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β- arrestin

" in MedChemExpress (MCE) Product Catalog:

68

Inhibitors & Agonists

17

Peptides

1

Recombinant Proteins

1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-119706
    Barbadin
    Maximum Cited Publications
    10 Publications Verification

    Apoptosis Arrestin Others
    Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .
    Barbadin
  • HY-111385
    UNC9994 hydrochloride
    1 Publications Verification

    Dopamine Receptor 5-HT Receptor Arrestin Neurological Disease
    UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
    UNC9994 hydrochloride
  • HY-120920

    Dopamine Receptor Inflammation/Immunology
    UNC9995 is a β-arrestin2-biased agonist of dopamine receptor Drd2. UNC9995 inhibits NLRP3 inflammasome activation by enhancing β-arrestin2-NLRP3 interaction, thus prevents neuronal degeneration. Futhermore, UNC9995 activates the Drd2/β-arrestin2 signaling to prevent inflammation-related genes transcription-induced by JAK/STAT3. UNC9995 improves depressive behavior in mouse model, and improves astrocytes dysfunctions .
    UNC9995
  • HY-155099

    Dopamine Receptor Arrestin G Protein-coupled Receptor Kinase (GRK) Neurological Disease
    FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin .
    FGH31
  • HY-117829

    Dopamine Receptor 5-HT Receptor Histamine Receptor Arrestin Neurological Disease
    UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity .
    UNC9994
  • HY-123813

    Arrestin Cancer
    CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .
    CCX-777
  • HY-149336

    Dopamine Receptor Neurological Disease
    D1R antagonist 1 (compound 12a) is a D1R antagonist, involved in G-protein- and β-arrestin-based signaling .
    D1R antagonist 1
  • HY-119486A

    (Rac)-PF-06649751; (Rac)-CVL-751

    Dopamine Receptor Arrestin Neurological Disease
    (Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity .
    (Rac)-Tavapadon
  • HY-122246

    GPR55 PKC ERK Arrestin Metabolic Disease
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
    ML192
  • HY-125020

    Others Inflammation/Immunology
    NCGC00135472 is a potent agonist of resolvin D1 receptor (DRV1), with the EC50 of 0.37 nM and 0.32 μM for β-arrestin and cAMP activities, respectively .
    NCGC00135472
  • HY-P2141A
    TRV-120027 TFA
    3 Publications Verification

    Angiotensin Receptor Arrestin 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 .
    TRV-120027 TFA
  • HY-P2141
    TRV-120027
    3 Publications Verification

    Angiotensin Receptor Arrestin 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 .
    TRV-120027
  • HY-15705

    GPR35 Arrestin Metabolic Disease Inflammation/Immunology
    GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca 2+ release assay, respectively .
    GPR35 agonist 2
  • HY-160187

    Others Cardiovascular Disease
    AAA is a potent blocker of 20-Hydroxyeicosatetraenoic acid (20-HETE) receptor that binds directly to GPR75 and prevents the increases in intracellular Ca2+, IP-1 and β-arrestin .
    AAA
  • HY-P2197

    Apelin Receptor (APJ) Arrestin Inflammation/Immunology
    ELA-11(human), a peptide, is a full agonist of human apelin receptor, with a pKi of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment .
    ELA-11(human)
  • HY-117295A

    Arrestin Inflammation/Immunology Cancer
    7-Fluorotryptamine hydrochloride is a potent agonist of GPRC5A. 7-Fluorotryptamine hydrochloride induces GPRC5A-mediated β-arrestin recruitment. 7-Fluorotryptamine hydrochloride can be used for research of immune and cancer signaling .
    7-Fluorotryptamine hydrochloride
  • HY-156157

    GPR55 Cancer
    GPR55 agonist 4 (Compound 28) is a GPR55 agonist (EC50: 131 nM, and 1.41 nM for hGPR55 and rGPR55). GPR55 agonist 4 induces β-arrestin recruitment to human GPR55 .
    GPR55 agonist 4
  • HY-161717

    Adenosine Receptor Cardiovascular Disease
    MRS5663 (Compound 3a) is an A3AR agonist, with an EC50 of 5.62 nM for β-arrestin2 recruitment assay. MRS5663 has a cytoprotective effect on skeletal muscle ischemia-reperfusion injury/claudication model .
    MRS5663
  • HY-160628

    Free Fatty Acid Receptor Metabolic Disease
    GPR120 Agonist 4 (example 1) is a GPR120 agonist,with the EC50 values of 1 μM and 0.35 μM for β-arrestin A and Calcium A. GPR120 Agonist 4 can be used for the research of type II diabetes mellitus .
    GPR120 Agonist 4
  • HY-145600

    Opioid Receptor Arrestin Neurological Disease
    Tegileridine is the potent agonist of opioid receptor (MOR). Tegileridine is an oxa spiro derivative which reduces the side effects mediated by β-arrestin. Tegileridine has the potential for the research of pains and pains-related diseases (extracted from patent WO2017063509A1) .
    Tegileridine
  • HY-156107

    GPR55 Cancer
    GPR55 agonist 3 (Compound 26) is a GPR55 agonist (EC50: 0.239 nM, and 1.76 nM for hGPR55 and rGPR55). GPR55 agonist 3 induces β-arrestin recruitment to human GPR55 (EC50: 6.2 nM) .
    GPR55 agonist 3
  • HY-100677

    CXCR Endocrinology
    VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
    VUF11207
  • HY-103254
    ML221
    5+ Cited Publications

    Arrestin Apelin Receptor (APJ) Neurological Disease
    ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC50s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.
    ML221
  • HY-147751

    Arrestin Apelin Receptor (APJ) Cardiovascular Disease
    APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with Ki of 1.3 μM. APJ receptor agonist 6 has EC50 values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively .
    APJ receptor agonist 6
  • HY-150056

    Cannabinoid Receptor Arrestin Neurological Disease
    CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC50 values of 0.018 μM and 1.241 μM, respectively .
    CB1R Allosteric modulator 3
  • HY-P5017

    Oxytocin Receptor Endocrinology
    (Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR) .
    (Val3,Pro8)-Oxytocin
  • HY-14299
    Indacaterol
    4 Publications Verification

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
    Indacaterol
  • HY-P2249

    Arrestin Apelin Receptor (APJ) Cardiovascular Disease
    ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
    ELA-21 (human)
  • HY-110302

    Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
    6'-GNTI dihydrochloride
  • HY-150057

    Cannabinoid Receptor Others
    CB1R Allosteric modulator 4 is a positive allosteric modulator of cannabinoid type-1 (CB1R) with good biological activity. CB1R Allosteric modulator 4 inhibits cAMP production and shows robust activity in β-arrestin-2 recruitment .
    CB1R Allosteric modulator 4
  • HY-149337

    Dopamine Receptor Neurological Disease
    D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
    D3R ligand 1
  • HY-14299A
    Indacaterol maleate
    4 Publications Verification

    QAB149

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
    Indacaterol maleate
  • HY-113689

    Cannabinoid Receptor Neurological Disease
    GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
    GAT211
  • HY-108742
    Abaloparatide
    1 Publications Verification

    BA 058; BIM 44058

    Thyroid Hormone Receptor Arrestin Metabolic Disease
    Abaloparatide (BA 058) is a parathyroid hormone receptor 1 (PTHR1) analog. Abaloparatide also is a selective PTHR1 activator. Abaloparatide enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide enhances bone formation and cortical structure in mice. Abaloparatide has the potential for the research of osteoporosis .
    Abaloparatide
  • HY-108656A

    P2Y Receptor Arrestin Cardiovascular Disease
    MRS2365 trisodium is a potent and selective P2Y1 receptor (EC50=0.4 nM)/[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity .
    MRS2365 trisodium
  • HY-138951

    Protease Activated Receptor (PAR) Inflammation/Immunology Cancer
    AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca 2+ release .
    AY77
  • HY-163277

    Opioid Receptor Inflammation/Immunology
    PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC50 of 1.1 nM and exhibits lowβ-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .
    PIPE-3297
  • HY-W010907

    GPR35 ERK Neurological Disease
    Pamoic acid disodium is a potent GPR35 agonist with an EC50 value of 79 nM. Pamoic acid disodium induces GPR35 internalization and activates ERK1/2 with EC50 values of 22 nM and 65 nM, respectively. Pamoic acid disodium potently recruits β-arrestin2 to GPR35 and has an antinociceptive effect .
    Pamoic acid disodium
  • HY-P1102
    TC14012
    2 Publications Verification

    CXCR HIV Infection Cancer
    TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity .
    TC14012
  • HY-P2197A

    Apelin Receptor (APJ) Inflammation/Immunology
    ELA-11(human) TFA is a high affinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
    ELA-11(human) TFA
  • HY-14299R

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol (Standard) is the analytical standard of Indacaterol. This product is intended for research and analytical applications. Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
    Indacaterol (Standard)
  • HY-108742A
    Abaloparatide TFA
    1 Publications Verification

    BA 058 TFA; BIM 44058 TFA

    Thyroid Hormone Receptor Arrestin Metabolic Disease Endocrinology
    Abaloparatide TFA (BA 058 TFA) is a parathyroid hormone receptor 1 (PTHR1) analogue. Abaloparatide TFA also is a selective PTHR1 activator. Abaloparatide TFA enhances Gs/cAMP signaling and β-arrestin recruitment. Abaloparatide TFA enhances bone formation and cortical structure in mice. Abaloparatide TFA has the potential for the research of osteoporosis .
    Abaloparatide TFA
  • HY-P1102A

    CXCR HIV Infection Cancer
    TC14012 TFA, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 TFA is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 TFA has anti-HIV activity and anti-cancer activity .
    TC14012 TFA
  • HY-145278

    RXFP Receptor Neurological Disease
    RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC50=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC50 values in the range of 10-22 nM .
    RXFP3/4 agonist 2
  • HY-157429

    5-HT Receptor Neurological Disease
    25N-N1-Nap (compound 16) is a β-arrestin-biased 5-HT2A agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6 J mice .
    25N-N1-Nap
  • HY-14299AR

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
    Indacaterol maleate (Standard)
  • HY-155183

    Adenosine Receptor Inflammation/Immunology Cancer
    A3AR agonist 1 (Compound 12) is an A3AR agonist (Ki: 25.8 nM). A3AR agonist 1 stimulates β-arrestin2 recruitment, with an EC50 value of 5.17 nM. A3AR agonist 1 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, etc .
    A3AR agonist 1
  • HY-P2106
    Elabela(19-32)
    3 Publications Verification

    Arrestin Apelin Receptor (APJ) Cardiovascular Disease
    Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
    Elabela(19-32)
  • HY-120645

    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-162495

    CCR Inflammation/Immunology
    IDOR-1117-2520 is a potent and selective antagonist of CCR6. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 can be used for research of autoimmune diseases .
    IDOR-1117-2520

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