Search Result

Results for "

β-arrestin recruitment

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (22) 5-HT Receptor (7) Adenosine Receptor (3) Apelin Receptor (APJ) (5) Cannabinoid Receptor (2) CCR (1) CXCR (12) Dopamine Receptor (9) EBI2/GPR183 (1) ERK (1) Free Fatty Acid Receptor (2) GLP Receptor (1) GPR35 (1) GPR55 (2) Histamine Receptor (1) HIV (2) Hydroxycarboxylic Acid Receptor (HCAR) (1) Interleukin Related (1) mAChR (1) Mas-related G-protein-coupled Receptor (MRGPR) (1) Opioid Receptor (10) P2Y Receptor (2) PERK (1) Prostaglandin Receptor (1) Protease Activated Receptor (PAR) (1) PTHR (2)
By Research Areas:	Cancer (17) Cardiovascular Disease (6) Endocrinology (3) Infection (2) Inflammation/Immunology (17) Metabolic Disease (5) Neurological Disease (29)

By Targets:

Arrestin (22)

5-HT Receptor (7)

Adenosine Receptor (3)

Apelin Receptor (APJ) (5)

Cannabinoid Receptor (2)

CCR (1)

CXCR (12)

Dopamine Receptor (9)

EBI2/GPR183 (1)

ERK (1)

Free Fatty Acid Receptor (2)

GLP Receptor (1)

GPR35 (1)

GPR55 (2)

Histamine Receptor (1)

HIV (2)

Hydroxycarboxylic Acid Receptor (HCAR) (1)

Interleukin Related (1)

mAChR (1)

Mas-related G-protein-coupled Receptor (MRGPR) (1)

Opioid Receptor (10)

P2Y Receptor (2)

PERK (1)

Prostaglandin Receptor (1)

Protease Activated Receptor (PAR) (1)

PTHR (2)

By Research Areas:

Cancer (17)

Cardiovascular Disease (6)

Endocrinology (3)

Infection (2)

Inflammation/Immunology (17)

Metabolic Disease (5)

Neurological Disease (29)

Inhibitors & Agonists

Peptides

Targets Recommended: Arrestin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-128121

MLS1547	Dopamine Receptor	Neurological Disease
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (K_i=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-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-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-117829

UNC9994 1 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-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 .

HY-176446

Mrgx2 antagonist-3	Mas-related G-protein-coupled Receptor (MRGPR)	Inflammation/Immunology
Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of MrgX2 receptor with an IC₅₀ value of 0.042-2.5 nM. Mrgx2 antagonist-3 blocks downstream G protein signaling and β-Arrestin recruitment, thereby inhibiting MrgX2 receptor-mediated calcium influx and cellular degranulation. Mrgx2 antagonist-3 is promising for research of inflammation-related diseases and pruritus, such as chronic urticaria, allergic asthma .

HY-123813

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

HY-159177

M4 mAChR Modulator-1	mAChR	Neurological Disease
M4 mAChR Modulator-1 (compound 23i) is a M4 mAChR positive allosteric modulator (PAM). M4 mAChR Modulator-1 exhibits significantly greater cooperativity with ACh in β-arrestin recruitment over G protein activation. M4 mAChR Modulator-1 displays weak PAM effect in G protein-mediated responses, but strong PAM effect in β-arrestin recruitment .

HY-175504

MLS6357	Dopamine Receptor PERK	Neurological Disease
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .

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-175505

Dopamine D3 receptor antagonist-3	Dopamine Receptor	Neurological Disease
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC₅₀ and a K_d of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .

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-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 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-115615

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

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-141434

5-OxoETE methyl ester	Hydroxycarboxylic Acid Receptor (HCAR)	Inflammation/Immunology Cancer
5-OxoETE methyl ester is the agonist for oxoeicosanoid receptor 1 (OXER1). 5-OxoETE methyl ester binds to OXER1, and activates downstream signaling pathways **β-arrestin recruitment with an EC₅₀** of 1.54 µM .

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-161717

MRS5663	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 .

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-122197

ML339 3 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-169841

IHCH-7086	5-HT Receptor	Neurological Disease
IHCH-7086 is a β-arrestin-biased 5-HT_2A serotonin receptor agonist (K_i: 12.59 nM). IHCH-7086 recruits β-arrestin through activation of 5-HT2A receptors, thereby removing hallucinogenic activity. IHCH-7086 improves depression-like behavior in mice without hallucinogenic effects .

HY-W664041

Noncatechol agonist-1	Dopamine Receptor	Neurological Disease
Noncatechol agonist-1 (19) is a Noncatechol agonist with full efficacy at both D1R-G protein and D1R-β-arrestin2 pathways, with pEC₅₀ values of 8.41 for D1R-mediated cAMP production and 7.7 for β-arrestin2 recruitment, respectively .

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-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-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-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-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 .

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-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 low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

HY-162728

RO-76	Opioid Receptor	Neurological Disease
RO-76 is a mu opioid receptor (μOR) selective partial agonist. RO-76 binds to μOR-G-protein complex with an EC₅₀ value of 454 nM. RO-76 reduces β-Arrestin-1/2 recruitment. RO-76 shows antinociception activity .

HY-108742

Abaloparatide 2 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-P1102

TC14012 3 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-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-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-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-108742A

Abaloparatide TFA 2 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-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-155183

A3AR agonist 1	Adenosine Receptor	Inflammation/Immunology Cancer
A3AR agonist 1 (Compound 12) is an A3AR agonist (K_i: 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 .

HY-172541

LN6023 hydrochloride	CXCR	Cardiovascular Disease
LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC₅₀ = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis .

HY-178103

D1R antagonist 2	Dopamine Receptor Arrestin	Neurological Disease
D1R antagonist 2 (Compound 13a) is a BBB-penetrable D1R antagonist with IC₅₀s of 35.6 and 70 nM for cAMP-based D1R and *β-arrestin*-based D1R, respectively. D1R antagonist 2 effectively antagonizes D1R-mediated cAMP and β-arrestin recruitment. D1R antagonist 2 can be used for neurodegenerative and neuropsychiatric diseases such as schizophrenia, Parkinson’s disease and Alzheimer’s disease research .

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-162495

IDOR-1117-2520	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 .

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-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-119234

CX4338	CXCR	Inflammation/Immunology
CX4338 is a CXCL8-mediated chemokine inhibitor with the activity of inhibiting CXCR2-mediated cell migration. CX4338 selectively inhibits CXCR2-mediated β-arrestin-2 recruitment and receptor internalization while enhancing CXCR2-mediated MAPK activation. CX4338 also inhibited CXCL8-induced chemotaxis, showing efficacy in CXCR2-overexpressing cells and human neutrophils. In vivo, CX4338 significantly reduced LPS-induced neutrophil numbers in mouse bronchoalveolar lavage fluid. The mechanism of action of CX4338 is to selectively inhibit CXCR2-mediated β-arrestin-2 activation, which is sufficient to inhibit CXCL8-mediated chemotaxis .

HY-178323

MW073	5-HT Receptor Arrestin	Neurological Disease
MW073 is a highly selective and orally active 5-HT2BR antagonist (IC₅₀ =70 nM). MW073 exerts its effects by concentration-dependently inhibiting receptor activity and *β-arrestin-1* recruitment. MW073 ameliorates synaptic plasticity and behavioral deficits, including aggression, in Alzheimer’s disease (AD) mouse models. MW073 can be used for Alzheimer’s disease (AD) research ^[1][2].

HY-175231

ST171	5-HT Receptor	Neurological Disease
ST171 is a bitopic 5-HT1AR agonist with an K_i of 0.41  nM. ST171 selectively activates G_i/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without G_s activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .

HY-174466

5-HT2AR ligand 1	5-HT Receptor Arrestin	Neurological Disease
5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT_2AR ligand with nanomolar affinity for 5-HT_2AR (K_i: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases .

Cat. No.	Product Name	Target	Research Area