2. Signaling Pathways
  3. GPCR/G Protein
  4. Arrestin

Arrestin

 
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-119706
    Barbadin
    		Inhibitor 98.93%
    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-103254
    ML221
    		Inhibitor 99.55%
    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-122197
    ML339
    		Antagonist 99.88%
    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 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. 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-108742A
    Abaloparatide TFA
    		Activator 99.86%
    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-117295A
    7-Fluorotryptamine hydrochloride
    		98.86%
    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-W018158
    DHICA
    DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of true black pigment, and it’s also a moderately potent GPR35 agonist. DHICA shows an ability to stimulate β-arrestin translocation signaling with an EC50 value of 23.2 μM in the U2OS cell line. DHICA plays a significant role in promoting and protecting against DNA damage.
    DHICA
  • HY-P1682A
    Balixafortide TFA
    		Inhibitor 99.78%
    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-111385
    UNC9994 hydrochloride
    		Agonist 98.83%
    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-108742
    Abaloparatide
    		Activator 99.94%
    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-P2141
    TRV-120027
    		Agonist 99.46%
    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-P2106
    Elabela(19-32)
    		Activator 99.64%
    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-P2106A
    Elabela(19-32) TFA
    		Activator 98.78%
    Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart.
    Elabela(19-32) TFA
  • HY-P2141A
    TRV-120027 TFA
    		Agonist 99.69%
    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-119486A
    (Rac)-Tavapadon
    		Agonist 99.87%
    (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-123813
    CCX-777
    		Agonist 98.73%
    CCX-777 is a partial agonist of β-arrestin-2 recruitment to ACKR3 (atypical chemokine receptor 3).
    CCX-777
  • HY-P2249
    ELA-21 (human)
    		Activator 98.92%
    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-P2197
    ELA-11(human)
    		Inhibitor 99.03%
    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-122246
    ML192
    		Inhibitor
    ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.
    ML192
  • HY-15705
    GPR35 agonist 2
    		Inhibitor 98.84%
    GPR35 agonist 2 (compound 11) is a potent agonist of GPR35, with EC50s of 26 and 3.2 nM in the β-arrestin and Ca2+ release assay, respectively.
    GPR35 agonist 2
  • HY-117829
    UNC9994
    		Agonist 98.06%
    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
Cat. No. Product Name / Synonyms Application Reactivity