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Results for "

β-arrestin recruitment

" in MedChemExpress (MCE) Product Catalog:

31

Inhibitors & Agonists

10

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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) .
    MLS1547
  • 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 .
    BMS-986122
  • HY-156157
    GPR55 agonist 4

    		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-156107
    GPR55 agonist 3

    		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-P1682
    Balixafortide

    POL6326

    		 CXCR Arrestin Cancer
    Balixafortide (POL6326) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
    Balixafortide
  • HY-P1682A
    Balixafortide TFA
    1 Publications Verification

    POL6326 TFA

    		 CXCR Arrestin Cancer
    Balixafortide TFA (POL6326 TFA) is a potent, selective, well-tolerated peptidic CXCR4 antagonist with an IC50 < 10 nM. Balixafortide TFA shows 1000-fold selective for CXCR4 than a large panel of receptors including CXCR7. Balixafortide TFA blocks β-arrestin recruitment and calcium flux with IC50s < 10 nM. Balixafortide TFA is also a potent hematopoietic stem and progenitor cell (HSPC) mobilizing agent. Anti-cancer effects .
    Balixafortide TFA
  • HY-117829
    UNC9994

    		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
    CCX-777

    		Arrestin Cancer
    CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3) .
    CCX-777
  • HY-119486A
    (Rac)-Tavapadon

    (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-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-P2197
    ELA-11(human)

    		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
    7-Fluorotryptamine hydrochloride

    		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-P2249
    ELA-21 (human)

    		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
    6'-GNTI dihydrochloride

    		Opioid Receptor Neurological Disease
    6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .
    6'-GNTI dihydrochloride
  • HY-150057
    CB1R Allosteric modulator 4

    		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-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-138951
    AY77

    		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
    PIPE-3297

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

    		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
    ELA-11(human) TFA

    		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-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
    TC14012 TFA

    		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-155183
    A3AR agonist 1

    		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-118140
    ZCZ011

    		Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
    ZCZ011
  • HY-122197
    ML339

    		CXCR Apelin Receptor (APJ) Arrestin Cancer
    ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 has no inhibitory effect on CXCR5，CXCR4，CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research .
    ML339
  • HY-155184
    A3AR agonist 2

    		Adenosine Receptor Neurological Disease Inflammation/Immunology Cancer
    A3AR agonist 2 (Compound 19) a selective A3AR agonist (Ki: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC50 value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions . A3AR agonist 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    A3AR agonist 2
  • HY-157425
    5-HT2CR agonist 1

    		5-HT Receptor Neurological Disease
    5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
    5-HT2CR agonist 1
  • HY-P3346
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)

    		Apelin Receptor (APJ) Cardiovascular Disease
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki of 0.6 nM. NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) can activate Gαi1 (EC50=0.8 nM) and recruit β-arrestin2 (EC50=31 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) exhibits prolonged cardiac effects .
    NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)
  • HY-108656A
    MRS2365 trisodium

    		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-108656
    MRS2365

    		P2Y Receptor Arrestin Cardiovascular Disease
    MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors .
    MRS2365

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