Search Result

Results for "

β- arrestin

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (55) 5-HT Receptor (12) Adenosine Receptor (4) Adenylate Cyclase (1) Adrenergic Receptor (11) Angiotensin Receptor (2) Apelin Receptor (APJ) (13) Apoptosis (1) Calcium Channel (5) Cannabinoid Receptor (8) Caspase (1) CaSR (1) CCR (2) Complement System (2) CXCR (21) DNA/RNA Synthesis (2) Dopamine Receptor (21) Drug Derivative (3) Drug Intermediate (2) Drug Isomer (1) EBI2/GPR183 (1) Endogenous Metabolite (3) Epigenetic Reader Domain (1) ERK (6) Formyl Peptide Receptor (FPR) (1) Free Fatty Acid Receptor (3) G protein-coupled Bile Acid Receptor 1 (2) G Protein-coupled Receptor Kinase (GRK) (1) GHSR (2) GLP Receptor (3) GPR119 (1) GPR35 (6) GPR39 (1) GPR55 (3) GPR84 (2) Histamine Receptor (3) HIV (2) Hydroxycarboxylic Acid Receptor (HCAR) (1) iGluR (2) Interleukin Related (3) Isotope-Labeled Compounds (2) LPL Receptor (2) mAChR (1) Mas-related G-protein-coupled Receptor (MRGPR) (4) Melatonin Receptor (1) Molecular Glues (1) Neurotensin Receptor (3) Opioid Receptor (14) Oxytocin Receptor (1) P-glycoprotein (2) P2Y Receptor (2) p38 MAPK (1) PERK (4) PKA (1) PKC (1) Potassium Channel (1) PPAR (1) Prostaglandin Receptor (2) Protease Activated Receptor (PAR) (1) PTHR (2) Reactive Oxygen Species (ROS) (1) Reference Standards (4) RXFP Receptor (2) Serotonin Transporter (1) SOD (2) Sodium Channel (2) TNF Receptor (1) Transmembrane Glycoprotein (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (34) Cardiovascular Disease (29) Endocrinology (11) Infection (2) Inflammation/Immunology (42) Metabolic Disease (20) Neurological Disease (65)
Click Chemistry:	Alkynes (3)

161

Inhibitors & Agonists

Peptides

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Click Chemistry

Targets Recommended: Arrestin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-119706

Barbadin Maximum Cited Publications 16 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 .

HY-122197

ML339 4 Publications Verification	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 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 .

HY-108742

Abaloparatide 3 Publications Verification BA 058; BIM 44058	PTHR Arrestin	Metabolic Disease Cancer
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 .

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.

HY-14299

Indacaterol 5 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 .

HY-P2141

TRV-120027 3 Publications Verification TRV027	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-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-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 .

HY-14299A

Indacaterol maleate 5 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 .

HY-145404

Mitragynine pseudoindoxyl 1 Publications Verification	Opioid Receptor	Metabolic Disease
Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, K_i=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, K_i=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, K_i=24 nM) and does not recruit *β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin*-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .

HY-120645

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

HY-122246

ML192	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 .

HY-P1102

TC14012 4 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 .

HY-P2106

Elabela(19-32) Maximum Cited Publications 6 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 G_αi1 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 .

HY-136390

ML417 1 Publications Verification	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-111385

UNC9994 hydrochloride 2 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 K_i of 79 nM for D₂R. UNC9994 hydrochloride is also an antagonist of G_i-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .

HY-W010907

Pamoic acid disodium 4 Publications Verification	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 .

HY-19835

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

HY-117829

UNC9994 2 Publications Verification	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 G_i-regulated cAMP production. Antipsychotic Activity .

HY-120920

UNC9995	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 .

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 .

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 pK_i of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment .

HY-100677

VUF11207 3 Publications Verification	CXCR	Endocrinology
VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pK_i of 8.1) ligand that induces recruitment of *β-arrestin2* (pEC₅₀ of 8.8) and subsequent internalization (pEC₅₀ of 7.9) of CXCR7 .

HY-108742A

Abaloparatide TFA 3 Publications Verification BA 058 TFA; BIM 44058 TFA	Arrestin PTHR	Metabolic Disease Endocrinology Cancer
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 .

HY-P2106A

Elabela(19-32) TFA Maximum Cited Publications 6 Publications Verification	Apelin Receptor (APJ) Arrestin	Cardiovascular Disease
Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the G_αi1 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 .

HY-15705

GPR35 agonist 2	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 .

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 .

HY-P10333A

LIH383 TFA	CXCR	Neurological Disease Inflammation/Immunology
LIH383 TFA is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 TFA efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling .

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) .

HY-P2249

ELA-21 (human)	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
ELA-21 (human) is an apelin receptor agonist with a pK_i 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 .

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 .

HY-14299AR

Indacaterol maleate (Standard) QAB149 (Standard)	Reference Standards 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 .

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 .

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 ?-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-155480

PSB-22034	Mas-related G-protein-coupled Receptor (MRGPR)	Inflammation/Immunology
PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca ²⁺ and β-arrestin experiments, respectively .

HY-136960

β2AR antagonist 1	Adrenergic Receptor	Others
β2AR antagonist 1 is a potent β2-adrenergic receptor (β2AR) inhibitor. β2AR antagonist 1 exhibits high selectivity for β2AR over β1AR, vasopressin receptor type 2, and angiotensin type 1 receptor. β2AR antagonist 1 stabilizes the inactive conformation of β2AR and interferes with its coupling to G proteins and β-arrestins .

HY-147751

APJ receptor agonist 6	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i 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 .

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-14299R

Indacaterol (Standard)	Reference Standards 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 .

HY-145278

RXFP3/4 agonist 2	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 .

HY-117533

UNC0006	Dopamine Receptor	Neurological Disease
UNC0006 is a β-arrestin-biased dopamine D2 ligand. UNC0006 can be used in the study of antipsychotic .

HY-172995

RS130-180	5-HT Receptor	Neurological Disease
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT_2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .

HY-179226

AP-7-168	Molecular Glues Adrenergic Receptor	Inflammation/Immunology
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma .

HY-175306

GPR183 inverse agonist-1	EBI2/GPR183 Arrestin	Inflammation/Immunology Cancer
GPR183 inverse agonist-1 (Compound 78) is a GPR183 inverse agonist. GPR183 inverse agonist-1 inhibits the GPR183-mediated Gi activation and *β-arrestin2* recruitment, and blocks PBMC migration. GPR183 inverse agonist-1 can be used for inflammatory, autoimmune and neoplastic disorders research .

HY-155099

FGH31	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 K_i of 1.6 nM. FGH31 partial activates β- arrestin .

HY-179471

PSB-17365	GPR84	Inflammation/Immunology
PSB-17365 is a potent GPR84 agonist with EC₅₀ values of 2.5 nM and 100 nM in a cAMP accumulation assay and a β-arrestin 2 recruitment assay, respectively .

HY-175001

D1/D5 Receptor agonist-1	Dopamine Receptor Arrestin	Neurological Disease
D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in *β-arrestin* recruitment, with EC₅₀s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a K_i of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits *β-arrestin* signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease .

HY-123534

CYT-1010	Opioid Receptor	Neurological Disease
CYT-1010 is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC₅₀s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .

HY-123534A

CYT-1010 hydrochloride	Opioid Receptor	Neurological Disease
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC₅₀s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively .

HY-175366

DOR agonist 3	Opioid Receptor Arrestin	Neurological Disease
DOR agonist 3 (Compound 10) is a δ-opioid receptor (DOR)-selective positive allosteric modulator. DOR agonist 3 enhances G protein signaling while reducing β-arrestin2 recruitment. DOR agonist 3 is promising for research of chronic pain and depression .

HY-113689

GAT211	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 .

Cat. No.	Product Name	Target	Research Area

HY-108742

Abaloparatide 3 Publications Verification BA 058; BIM 44058	PTHR Arrestin	Metabolic Disease Cancer
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 .

HY-P3419

PAMP-12 (unmodified) 2 Publications Verification	Mas-related G-protein-coupled Receptor (MRGPR) PERK Calcium Channel	Cardiovascular Disease Inflammation/Immunology
PAMP-12 (unmodified) is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) can reduce cAMP accumulation, increase Ca ²⁺levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) can be used for the research of hypotension and ulcerative colitis .

HY-P2141

TRV-120027 3 Publications Verification TRV027	Angiotensin Receptor Arrestin	Cardiovascular Disease
TRV120027, a *β-arrestin-1*-biased agonist of the angiotensin II receptor type 1 (AT1R), engages β-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-P1102

TC14012 4 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 .

HY-P2106

Elabela(19-32) Maximum Cited Publications 6 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 G_αi1 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 .

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 .

HY-P1682

Balixafortide 1 Publications Verification 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 .

HY-12557

γ-Glutamylvaline γ-Glu-Val	Endogenous Metabolite CaSR Wnt TNF Receptor Interleukin Related PPAR β-catenin	Inflammation/Immunology
γ‑Glutamylvaline (γ-Glu-Val) is a calcium‑sensing receptor (CaSR) agonist. γ‑Glutamylvaline activates CaSR and facilitates its binding to β‑arrestin 2 to modulate inflammatory and metabolic homeostasis signaling. γ‑Glutamylvaline inhibits TNF‑α‑induced IL‑6/MCP‑1 and enhances adiponectin/PPARγ in adipocytes. γ‑Glutamylvaline upregulates Wnt5a, restores *β‑catenin* phosphorylation, and reduces serine‑phosphorylated IRS‑1 in adipocytes. γ-Glutamylvaline can be used for the research of low-grade chronic inflammation .

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 pK_i of 7.85. ELA-11(human) completely inhibits Forskolin-induced cAMP production and stimulates *β-arrestin* recruitment .

HY-108742A

Abaloparatide TFA 3 Publications Verification BA 058 TFA; BIM 44058 TFA	Arrestin PTHR	Metabolic Disease Endocrinology Cancer
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 .

HY-P2106A

Elabela(19-32) TFA Maximum Cited Publications 6 Publications Verification	Apelin Receptor (APJ) Arrestin	Cardiovascular Disease
Elabela(19-32) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the G_αi1 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 .

HY-P10333A

LIH383 TFA	CXCR	Neurological Disease Inflammation/Immunology
LIH383 TFA is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 TFA efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling .

HY-P2249

ELA-21 (human)	Arrestin Apelin Receptor (APJ)	Cardiovascular Disease
ELA-21 (human) is an apelin receptor agonist with a pK_i 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 .

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 ?-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-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 .

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 .

HY-P11246

A13:B7-24-GG	RXFP Receptor	Metabolic Disease
A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a K_i value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (K_i = 602.56 nM) and an inhibitory effect on cAMP (EC₅₀) of 1.17 nM. Activation of RXFP4 by A13:B7-24-GG leads to the recruitment of β-Arrestin2, with an EC₅₀ of 22.39 nM. A13:B7-24-GG can be used for research on chronic constipation .

HY-P10333

LIH383	CXCR	Neurological Disease Inflammation/Immunology
LIH383 is an agonist of ACKR3 (CXCR7) (EC₅₀=0.61 nM). LIH383 efficiently induces the recruitment of β-arrestin to ACKR3 but does not trigger typical G protein signaling .

HY-P5017

(Val3,Pro8)-Oxytocin	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) .

HY-P2197A

ELA-11(human) TFA	Apelin Receptor (APJ)	Inflammation/Immunology
ELA-11(human) TFA is a high affinity apelin receptor agonist (K_i=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.

HY-P3419A

PAMP-12 (unmodified) TFA	Mas-related G-protein-coupled Receptor (MRGPR) PERK Calcium Channel	Cardiovascular Disease Inflammation/Immunology
PAMP-12 (unmodified) TFA is an endogenous peptide and is a MrgX2 agonist. PAMP-12 (unmodified) TFA can reduce cAMP accumulation, increase Ca ²⁺levels, enhance beta-arrestin recruitment, decrease IP-1, and increases phosphoERK. PAMP-12 (unmodified) TFA can elicit hypotension through inhibiting catecholamine secretion from sympathetic nerve endings and adrenal chromaffin cells. PAMP-12 (unmodified) TFA can be used for the research of hypotension and ulcerative colitis .

HY-P1345B

[DArg10, DAla20] TLQP-21	Complement System Calcium Channel Drug Derivative	Neurological Disease Metabolic Disease Inflammation/Immunology
[DArg10, DAla20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aR agonist (EC₅₀: 87 nM for β-arrestin recruitment). [DArg10, DAla20] TLQP-21 elicits calcium influx. [DArg10, DAla20] TLQP-21 slightly but not significantly potentiates adrenergic-induced lipolysis. [DArg10, DAla20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions .

HY-P1345C

[DArg10, Aib20] TLQP-21	Drug Derivative Complement System	Neurological Disease Metabolic Disease Inflammation/Immunology
[DArg10, Aib20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aRpartial agonist, C3aR functional antagonist (EC₅₀: 854 nM for β-arrestin recruitment). [DArg10, Aib20] TLQP-21 shows no significant calcium flux activity. [DArg10, Aib20] TLQP-21 shows no activity in potentiating adrenergic-induced lipolysis. [DArg10, Aib20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions .

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P7606

	*ARRB1/Beta-Arrestin* 1 Protein, Human (His)** 1 Publications Verification rHuARRB1/beta-arrestin 1, His; ARRB1, β-arrestin 1	Human	E. coli
	ARRB1/Beta-Arrestin 1 Protein, Human (His) expresses in E. coli with a His tag. ARRB1/beta-Arrestin 1, found in the hypothalamus (ARH) and in N-38 neurons, is a scaffolding protein organizing downstream signaling molecules and as an adaptor protein aiding in ER internalization after its activation.

Compare Products


Products	In-stock - + Add to Cart
Cat. No.
Species
Source
Tag
Accession
Gene ID
Molecular Weight
Purity
Endotoxin Level
Biological Activity
Appearance
Formulation
Storage & Stability
Shipping
Free Sample	Yes No
Size	* This product has been "discontinued". Optimized version of product available: / In-stock - + Add to Cart Get quote

Cat. No.	Product Name	Chemical Structure

HY-139938S

(±)11(12)-EET methyl ester-d11

(±)11(12)-EET-d₁₁ methyl ester (11,12-EET methyl ester-d₁₁) is the deuterium labeled (±)11(12)-EET methyl ester (HY-139938). (±)11(12)-EET methyl ester (11,12-EET-methyl ester) is a methylated derivative of 11,12-epoxyeicosatrienoic acid (11,12-EET) (HY-130494). (±)11(12)-EET methyl ester cannot induce β-arrestin recruitment of the G protein-coupled receptor GPR132. (±)11(12)-EET methyl ester fails to enhance the expression of hematopoietic stem and progenitor cell (HSPC) markers. (±)11(12)-EET methyl ester can be used as a negative control molecule to study the structure-function relationship of 11,12-EET, facilitating the analysis of the role of the oxygenated fatty acid-GPR132 signaling axis in hematopoiesis .

HY-179551S

(±)11(12)-EET-d11 Methyl ester

(±)11(12)-EET-d₁₁ Methyl ester is the deuterium labeled (±)11(12)-EET methyl ester (HY-139938). (±)11(12)-EET methyl ester is a methylated derivative of 11,12-epoxyeicosatrienoic acid (11,12-EET) (HY-130494). (±)11(12)-EET methyl ester cannot induce β-arrestin recruitment of the G protein-coupled receptor GPR132. (±)11(12)-EET methyl ester fails to enhance the expression of hematopoietic stem and progenitor cell (HSPC) markers. (±)11(12)-EET methyl ester can be used as a negative control molecule to study the structure-function relationship of 11,12-EET, facilitating the analysis of the role of the oxygenated fatty acid-GPR132 signaling axis in hematopoiesis.

Host:	Mouse (3) Rabbit (1)
Reactivity:	Human (4) Rat (2) Mouse (2)
Application:	IHC-P (2) ICC/IF (1) IF-Tissue (2) IP (1) IHC-F (1) WB (4) ELISA (1)
Isotype:	IgG (2) IgG2b (2)
Conjugation:	Non-conjugated (4)
Clonality:	Monoclonal (3)
Modification:	Unmodified (3)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P80569

	beta Arrestin 1 Antibody (YA822) ARB1; ARR1; ARRB1; ARRB1_HUMAN; arrestin 2; arrestin beta 1; arrestin beta-1; Beta-arrestin-1.	WB	Human
	beta Arrestin 1 Antibody (YA822) is a Mouse-derived and non-conjugated IgG2b monoclonal antibody, targeting to beta Arrestin 1.

HY-P80569A

	beta Arrestin 1 Antibody (YA822)(PBS only) ARB1; ARR1; ARRB1; ARRB1_HUMAN; arrestin 2; arrestin beta 1; arrestin beta-1; Beta-arrestin-1.	WB	Human
	beta Arrestin 1 Antibody (YA822) is a Mouse-derived and non-conjugated IgG2b monoclonal antibody, targeting to beta Arrestin 1.

HY-P85419

	Beta Arrestin 2 Antibody (YA5111) ARRB2; ARB2; ARR2; Beta-arrestin-2; arrestin beta-2	WB, IHC-P, ICC/IF, IP, ELISA, IF-Tissue	Human, Mouse, Rat
	Beta Arrestin 2 Antibody (YA5111) is a Mouse-derived and non-conjugated monoclonal antibody, targeting to Arrestin-β-2.

HY-P85544

	beta Arrestin 1 Antibody (YA5236) ARB 1; ARB 1; ARB1; ARB1; ARR 1; ARR 1; ARR1; ARR1; ARRB 1; ARRB1; ARRB1; ARRB1_HUMAN; arrestin 2; arrestin beta 1; arrestin beta-1; Beta-arrestin-1.	WB, IHC-P, IHC-F, IF-Tissue	Human, Mouse, Rat
	beta Arrestin 1 Antibody (YA5236) is a Rabbit-derived and non-conjugated monoclonal antibody, targeting to beta Arrestin 1.

Compare Products


Products	In-stock - + Add to Cart
Cat. No.
Host
Reactivity
Application
Dilution Ratio
Molecular Weight
Conjugation
Clonality
Immunogen
Appearance
Isotype
Gene ID
SwissProt ID
Purity
Formulation
Free Sample	Yes No
Size	* This product has been "discontinued". Optimized version of product available: / In-stock - + Add to Cart Get quote

Cat. No.	Product Name		Classification

HY-155480

PSB-22034		Alkynes
PSB-22034 (compound 30d) is a selective agonist of MRGPRX4 with EC₅₀s of 11.2 nM and 30.0 nM in Ca ²⁺ and β-arrestin experiments, respectively .

HY-172995

RS130-180		Alkynes
RS130-180 is a selective β-arrestin-biased agonist targeting the serotonin 2A receptor (5-HT_2aR). RS130-180 is promising for research of neuropsychiatric disorders such as depression .

HY-115643

AZ13581837		Alkynes
AZ13581837 is a GPR120 agonist with oral effectiveness, human EC₅₀ values of 5.2 nM, and mouse EC₅₀ of 4.3 nM. AZ13581837 signals through Gαq, Gαs, and β-arrestin pathways, reduces cAMP production, stimulates GLP-1 secretion, induces glucose lowering, and increases insulin secretion. AZ13581837 can be used for the research of type 2 diabetes .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: