Search Result

Results for "

Beta-arrestin recruitment

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (7) Adenosine Receptor (3) Adenylate Cyclase (1) Adrenergic Receptor (2) Apelin Receptor (APJ) (6) Arrestin (34) Calcium Channel (5) Cannabinoid Receptor (3) CCR (3) Complement System (2) CXCR (19) Dopamine Receptor (11) Drug Derivative (3) Drug Isomer (1) EBI2/GPR183 (1) Epigenetic Reader Domain (1) ERK (5) Formyl Peptide Receptor (FPR) (1) Free Fatty Acid Receptor (2) G protein-coupled Bile Acid Receptor 1 (2) GLP Receptor (2) GPR35 (1) GPR39 (1) GPR52 (1) GPR55 (2) GPR84 (2) Histamine Receptor (2) HIV (2) Hydroxycarboxylic Acid Receptor (HCAR) (1) iGluR (2) Interleukin Related (2) Isotope-Labeled Compounds (2) mAChR (1) Mas-related G-protein-coupled Receptor (MRGPR) (3) Neurotensin Receptor (2) Opioid Receptor (11) P-glycoprotein (2) P2Y Receptor (2) PERK (4) PKA (1) Potassium Channel (1) Prostaglandin Receptor (1) Protease Activated Receptor (PAR) (1) PTHR (2) RXFP Receptor (1) Serotonin Transporter (1) Sodium Channel (2) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (24) Cardiovascular Disease (16) Endocrinology (3) Infection (2) Inflammation/Immunology (29) Metabolic Disease (13) Neurological Disease (39)

By Targets:

5-HT Receptor (7)

Adenosine Receptor (3)

Adenylate Cyclase (1)

Adrenergic Receptor (2)

Apelin Receptor (APJ) (6)

Arrestin (34)

Calcium Channel (5)

Cannabinoid Receptor (3)

CCR (3)

Complement System (2)

CXCR (19)

Dopamine Receptor (11)

Drug Derivative (3)

Drug Isomer (1)

EBI2/GPR183 (1)

Epigenetic Reader Domain (1)

ERK (5)

Formyl Peptide Receptor (FPR) (1)

Free Fatty Acid Receptor (2)

G protein-coupled Bile Acid Receptor 1 (2)

GLP Receptor (2)

GPR35 (1)

GPR39 (1)

GPR52 (1)

GPR55 (2)

GPR84 (2)

Histamine Receptor (2)

HIV (2)

Hydroxycarboxylic Acid Receptor (HCAR) (1)

iGluR (2)

Interleukin Related (2)

Isotope-Labeled Compounds (2)

mAChR (1)

Mas-related G-protein-coupled Receptor (MRGPR) (3)

Neurotensin Receptor (2)

Opioid Receptor (11)

P-glycoprotein (2)

P2Y Receptor (2)

PERK (4)

PKA (1)

Potassium Channel (1)

Prostaglandin Receptor (1)

Protease Activated Receptor (PAR) (1)

PTHR (2)

RXFP Receptor (1)

Serotonin Transporter (1)

Sodium Channel (2)

Transmembrane Glycoprotein (1)

By Research Areas:

Cancer (24)

Cardiovascular Disease (16)

Endocrinology (3)

Infection (2)

Inflammation/Immunology (29)

Metabolic Disease (13)

Neurological Disease (39)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-160734

Aleniglipron GSBR-1290	GLP Receptor	Metabolic Disease
Aleniglipron (GSBR-1290) is an orally active glucagon-like peptide-1 receptor (GLP-1R) agonist, with an EC₅₀ value of less than 0.1 nM in HDB cell lines in cAMP stimulation assays. Aleniglipron selectively activates the Gαs-cAMP signaling pathway of GLP-1R without β-arrestin recruitment. Aleniglipron induces insulin release, promotes glucose clearance, reduces food intake and decreases body weight. Aleniglipron is applicable to research related to type 2 diabetes and obesity .

HY-175701

CT-996 RO7795081; RG6652	Arrestin GLP Receptor	Metabolic Disease
CT-996 is an orally active GLP-1RA agonist with an EC₅₀ of 0.49 nM. CT-996 reduces the recruitment of *β-arrestin* and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity .

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-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-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-162495

IDOR-1117-2520	CCR Calcium Channel Arrestin P-glycoprotein	Inflammation/Immunology Cancer
IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. 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 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation .

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-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-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-19867A

Burixafor hydrobromide TG-0054 hydrobromide	CXCR	Cardiovascular Disease Cancer
Burixafor (TG-0054) hydrobromide is a potent CXCR4 antagonist with a pIC₅₀ of 7.4. Burixafor hydrobromide inhibits the binding of CXCL12 to CXCR4, antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, and blocks the downstream Gαᵢ-mediated inhibitory effect on cAMP signal transduction. Burixafor hydrobromide mobilizes CD34 ⁺ hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor hydrobromide can be used for research on autologous hematopoietic stem cell transplantation (ASCT) .

HY-136832

Noribogaine hydrochloride	Serotonin Transporter Potassium Channel Arrestin Opioid Receptor	Cardiovascular Disease Neurological Disease
Noribogaine hydrochloride is an orally active, blood-brain barrier permeable SERT inhibitor (IC₅₀=50-300 nM) and hERG channel blocker. Noribogaine hydrochloride enhances serotonergic transmission, activates the κ-opioid receptor (OPRK) G protein signaling pathway and inhibits *β-arrestin* recruitment. Meanwhile, Noribogaine hydrochloride blocks the μ-opioid receptor (OPRM) signaling pathway as well as ion channels associated with cardiac repolarization. Noribogaine hydrochloride induces neuritogenesis, upregulates GDNF mRNA expression, and modulates opioid tolerance. Noribogaine hydrochloride reduces alcohol-seeking behavior in experimental animals, and is widely used in studies related to depression, addiction, alcoholism, and cardiotoxicity .

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-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-123813

CCX-777	CXCR Arrestin	Cancer
CCX-777 is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 is widely used in cancer-related research .

HY-164795

SBI-810	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 promotes the recruitment of *β-arrestin-2* to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 is applicable to research related to multiple pain disorders .

HY-164795A

SBI-810 hydrochloride	Neurotensin Receptor Arrestin iGluR ERK Sodium Channel	Neurological Disease
SBI-810 hydrochloride is a blood-brain barrier-permeable NTSR1 modulator. SBI-810 hydrochloride promotes the recruitment of *β-arrestin-2* to NTSR1 and antagonizes NTSR1-mediated Gq activation. SBI-810 hydrochloride inhibits excitatory synaptic transmission, NMDA receptor and extracellular signal-regulated kinase (ERK) signaling in spinal nociceptive neurons, reduces surface expression of Nav1.7 and action potential firing in primary sensory neurons, and attenuates C-fiber responses. SBI-810 hydrochloride effectively alleviates acute and chronic pain in various rodent models through peripheral and central modulation. SBI-810 hydrochloride is applicable to research related to multiple pain disorders .

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-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-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-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-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-163671

PW0729	GPR52 Arrestin	Neurological Disease
PW0729 is a selective GPR52 agonist. PW0729 activates G protein/cAMP signaling pathway, with bias toward this pathway over *β-arrestin* recruitment, and induces GPR52 desensitization. PW0729 can be used for the research of neuropsychiatric and neurological diseases .

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-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-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-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-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-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-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-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 .

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-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-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-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-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-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 .

Cat. No.	Product Name	Target	Research Area

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-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-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-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-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-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-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-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-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-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-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.	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.

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