Search Result

Results for "

β-arrestin recruitment

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Arrestin (14) 5-HT Receptor (3) Adenosine Receptor (3) Apelin Receptor (APJ) (5) Cannabinoid Receptor (2) CCR (1) CXCR (9) Dopamine Receptor (4) ERK (1) Free Fatty Acid Receptor (1) GPR35 (1) GPR55 (2) Histamine Receptor (1) HIV (2) Hydroxycarboxylic Acid Receptor (HCAR) (1) Interleukin Related (1) mAChR (1) Opioid Receptor (8) P2Y Receptor (2) Prostaglandin Receptor (1) Protease Activated Receptor (PAR) (1) PTHR (2)
By Research Areas:	Cancer (16) Cardiovascular Disease (5) Endocrinology (2) Infection (2) Inflammation/Immunology (14) Metabolic Disease (3) Neurological Disease (16)

By Targets:

Arrestin (14)

5-HT Receptor (3)

Adenosine Receptor (3)

Apelin Receptor (APJ) (5)

Cannabinoid Receptor (2)

CCR (1)

CXCR (9)

Dopamine Receptor (4)

ERK (1)

Free Fatty Acid Receptor (1)

GPR35 (1)

GPR55 (2)

Histamine Receptor (1)

HIV (2)

Hydroxycarboxylic Acid Receptor (HCAR) (1)

Interleukin Related (1)

mAChR (1)

Opioid Receptor (8)

P2Y Receptor (2)

Prostaglandin Receptor (1)

Protease Activated Receptor (PAR) (1)

PTHR (2)

By Research Areas:

Cancer (16)

Cardiovascular Disease (5)

Endocrinology (2)

Infection (2)

Inflammation/Immunology (14)

Metabolic Disease (3)

Neurological Disease (16)

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	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-123813

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

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-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-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-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-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-122197

ML339 1 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-100677

VUF11207	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-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 1 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 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 .

HY-W010907

Pamoic acid disodium 2 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-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 1 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-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-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-170342

KOR agonist 3	Opioid Receptor	Others
KOR agonist 3 (Compound 5) is a κ opioid receptor (κOR) agonist with an EC₅₀ of 0.88 nM. KOR agonist 3 also has a certain activation effect on μOR with an EC₅₀ of 720 nM. KOR agonist 3 shows no agonist activity for δOR at concentrations less than 1 μM. KOR agonist 3 has a lower ability to induce the recruitment of β-Arrestin-2 than U50488 (HY-15997B) .

HY-173052

SLW131	CXCR	Inflammation/Immunology
SLW131 (Compound 10) is the antagonist for CCR7 with a good affinity of K_i of 9.85 nM. SLW131 inhibits CCL19-induced Go protein activation with an IC₅₀ of 29.4 μM, inhibits β-arrestin2 recruitment with an IC₅₀ of 6.0 μM. SLW131 inhibits CCL19-induced cell morphological changes in primary BMDCs, and CCR7-mediated migration in mouse CD4+ T cell .

HY-171069

FFA2 agonist-1	Free Fatty Acid Receptor	Metabolic Disease
FFA2 agonist-1 (Compound 4) is the agonist for Free fatty acid receptor 2 (FFA2/GPR43) with an EC₅₀ of 81 nM. FFA2 agonist-1 exhibits activity in β-arrestin-2 recruitment assay and cAMP inhibition assay with EC₅₀ of 1.2 μM and 0.53 μM. FFA2 agonist-1 leads to appetite regulating peptide YY (PYY) mucosal responses, inhibits the fat accumulation, intestinal functions and food intake, and can be used for obesity research .

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-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-157425

5-HT2CR agonist 1	5-HT Receptor	Neurological Disease
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT_2CR partial agonist (E_max=71.09%) with an EC₅₀ value of 121.5 nM and no observed activity toward 5-HT_2AR or 5-HT_2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .

HY-155184

A3AR agonist 2	Adenosine Receptor	Neurological Disease Inflammation/Immunology Cancer
A3AR agonist 2 (Compound 19) a selective A3AR agonist (K_i: 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.

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 K_i 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 .

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-168351

Fluorphine	Opioid Receptor	Neurological Disease
Fluorphine is an analogue of Brorphine and can bind to μ-opioid receptor (MOR) (K_i: 12.5 nM). Fluorphine has GTPγS binding (EC₅₀: 75 nM) and βarrestin 2 recruitment (EC₅₀: 377 nM) activity. Fluorphine induces respiratory depressant effects .

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 .

HY-169859

EP4 receptor antagonist 7	Prostaglandin Receptor Interleukin Related	Inflammation/Immunology Cancer
EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC₅₀ value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC₅₀ value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD ⁸⁺ T cells into tumors in a CT26 murine colon cancer model .

Cat. No.	Product Name	Target	Research Area