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Pathways Recommended: Neuronal Signaling JAK/STAT Signaling
Results for "

β-arrestin signaling

" in MedChemExpress (MCE) Product Catalog:

55

Inhibitors & Agonists

9

Peptides

1

Natural
Products

2

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. 상품명 Target 연구분야 Chemical Structure
  • 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 .
    Aleniglipron
  • 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 .
    ML339
  • 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 .
    Abaloparatide
  • 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 .
    7-Fluorotryptamine hydrochloride
  • 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 .
    TRV-120027
  • 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, Ki=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, Ki=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, Ki=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 .
    Mitragynine pseudoindoxyl
  • HY-128121
    MLS1547

    		Dopamine Receptor Neurological Disease
    MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=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) .
    MLS1547
  • HY-165428
    SCH-900875

    		CXCR Arrestin Inflammation/Immunology
    SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease) .
    SCH-900875
  • 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 .
    ML417
  • 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 Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
    Elabela(19-32)
  • HY-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 .
    Noribogaine hydrochloride
  • 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) .
    Burixafor hydrobromide
  • HY-59132
    2-Amino-1-phenylethanol

    		Drug Intermediate Others
    2-Amino-1-phenylethanol is a pharmaceutical intermediate that can be used for the synthesis of antimalarial agents and β2-adrenergic receptor agonists .
    2-Amino-1-phenylethanol
  • 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 Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity .
    UNC9994 hydrochloride
  • HY-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 .
    SBI-810
  • 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 .
    SBI-810 hydrochloride
  • 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 .
    γ-Glutamylvaline
  • HY-16639
    ML314

    		GPR35 Neurotensin Receptor Neurological Disease Endocrinology
    ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
    ML314
  • HY-120511
    KNT-127
    1 Publications Verification

    		 Opioid Receptor Neurological Disease
    KNT-127 is a selective and BBB-penetrant δ-opioid receptor (DOR) agonist (Ki = 0.16 nM). KNT-127 is highly selective to the δ receptor, with Ki values of 0.16, 21.3 and 153 nM for δ, μ and κ receptors, respectively. KNT-127 acts as a biased ligand that mainly activates cyclic adenosine monophosphate (cAMP) signaling with lower beta-arrestin signaling activation. KNT-127 increases the release of dopamine and L-glutamate in the striatum, nucleus accumbens, and prefrontal cortex. KNT-127 exhibits antidepressant- and anxiolytic-like effects. KNT-127 can be studied in research on neurological diseases .
    KNT-127
  • 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 .
    Mrgx2 antagonist-3
  • 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 .
    UNC9995
  • 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 .
    Abaloparatide TFA
  • 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 Gαi1 and β-arrestin-2 signaling pathways with EC50s of 8.6 nM and 166 nM. Elabela(19-32) TFA induces receptor internalization and reduces arterial pressure, exerts positive inotropic effects on the heart .
    Elabela(19-32) TFA
  • HY-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 .
    PW0729
  • 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 .
    LIH383 TFA
  • 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 .
    6'-GNTI dihydrochloride
  • HY-175231
    ST171

    		5-HT Receptor Neurological Disease
    ST171 is a bitopic 5-HT1AR agonist with an Ki of 0.41  nM. ST171 selectively activates Gi/o signaling pathway and inhibits 5-HT1AR-mediated cAMP accumulation without Gs activation and marginal β-arrestin recruitment. T171 reduces hypersensitivity in chronic neuropathic and inflammatory pain mice model. ST171 can be used for pain research .
    ST171
  • 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 .
    TRV-120027 TFA
  • HY-10486
    JDTic

    		Opioid Receptor Neurological Disease
    JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal .
    JDTic
  • 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 Ki 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 .
    D1/D5 Receptor agonist-1
  • 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 .
    DOR agonist 3
  • 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 .
    PIPE-3297
  • 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 .
    LIH383
  • 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 .
    5-OxoETE methyl ester
  • HY-116445
    UNC9975

    		Dopamine Receptor Neurological Disease
    UNC9975 is a D2R agonist that displays signaling bias via β-arrestin–ergic signaling and a simultaneously antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9975 can be utilized in antipsychotic research .
    UNC9975
  • HY-153162A
    (-)-IHCH7041

    		Dopamine Receptor Neurological Disease
    (-)-IHCH7041 (Compound (-)-(S)-I-10) is a selective and orally active dopamine D2 receptor agonist with a Ki of 22.44 nM. (-)-IHCH7041 can activate Gαi1 protein and β-arrestin2 signaling pathway with EC50 values of 1.38 and 2.75 nM. (-)-IHCH7041 can improve cognitive impairment and memory capacity. (-)-IHCH7041 can be used for the research of neurological disease, such as Alzheimer's disease .
    (-)-IHCH7041
  • HY-149336
    D1R antagonist 1

    		Dopamine Receptor Neurological Disease
    D1R antagonist 1 (compound 12a) is a D1R antagonist, involved in G-protein- and β-arrestin-based signaling .
    D1R antagonist 1
  • HY-163345
    5-HT7R antagonist 2

    		5-HT Receptor Neurological Disease
    5-HT7R antagonist 2 (compound 4h) is a 5-HT7R antagonist that antagonizes the G protein and β-arrestin signaling pathways, with a Ki of 67 nM, the IC50 values in cAMP and Tango tests were 2.59 μM and 39.57 μM, respectively. 5-HT7R antagonist 2 has an effect on neurogenesis and can reduce repetitive behaviors related to autism spectrum disorder (ASD) and restore neurogenesis of ASD impairment .
    5-HT7R antagonist 2
  • HY-139938
    (±)11(12)-EET methyl ester

    11,12-EET methyl ester; (±)11,12-EpETrE methyl ester

    		 Drug Derivative Cardiovascular Disease Inflammation/Immunology
    (±)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 .
    (±)11(12)-EET methyl ester
  • HY-149337
    D3R ligand 1

    		Dopamine Receptor Neurological Disease
    D3R ligand 1 (compound 23b) is a potent and selective ligand of dopamine receptor D3R (Ki=66 nM), containing a THPB template. D3R ligand 1 is also an antagonist for both G-protein- and β-arrestin-based signaling .
    D3R ligand 1
  • HY-139938S
    (±)11(12)-EET methyl ester-d11

    11,12-EET methyl ester-d11; (±)11,12-EpETrE methyl ester-d11

    		 Isotope-Labeled Compounds Cardiovascular Disease Inflammation/Immunology
    (±)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 .
    (±)11(12)-EET methyl ester-d11
  • HY-183777
    B-007

    		Apelin Receptor (APJ) Arrestin Cardiovascular Disease
    B-007 is an AplnR agonist with G protein-biased signaling (EC50 = 11.6 nM). B-007 activates the G protein pathway while abolishing β-arrestin1 and β-arrestin2 signaling. B-007 serves as a scaffold for development of G protein-biased apelin receptor agonists. B-007 can be used for the research of heart failure .
    B-007
  • HY-120925
    TRV0109101

    		Opioid Receptor Arrestin Neurological Disease
    TRV0109101 is a μ-opioid peptide receptor (MOPR) selective agonist (KD = 70 nM) with blood-brain barrier permeability. TRV0109101 selectively promotes G protein signaling pathway coupling while reducing the recruitment of β-arrestin. TRV0109101 inhibits opioid-induced mechanical hyperalgesia and induces antinociceptive tolerance. TRV0109101 is applicable for pain-related research .
    TRV0109101
  • HY-165453
    VUF14480

    		Histamine Receptor Inflammation/Immunology
    VUF14480 is a partial agonist of histamine H4 (hH4) receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 binds covalently to hH4 receptor (pKi: 6.3 for hH4-WT receptor). VUF14480 partially induces hH4 receptor-mediated G protein activation and β-arrestin2 recruitment. VUF14480 can be used in the research of inflammatory diseases .
    VUF14480
  • HY-182850
    UCUF-965

    		CXCR Metabolic Disease
    UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment .
    UCUF-965
  • HY-47412
    Cariprazine impurity 1

    		Dopamine Receptor Neurological Disease
    Cariprazine impurity 1 is a dopamine D2 receptor (D2R) agonist. Cariprazine impurity 1 modulates D2R-mediated Gi/o signaling pathway to inhibit cAMP production, and regulates D2R-mediated β-arrestin2 recruitment pathway .
    Cariprazine impurity 1
  • HY-181822
    BMS-986331

    		Formyl Peptide Receptor (FPR) Arrestin PKA Interleukin Related Cardiovascular Disease
    BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC50 of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure .
    BMS-986331
  • HY-115643
    AZ13581837

    		GPR119 Arrestin GLP Receptor Metabolic Disease
    AZ13581837 is an orally active GPR120 agonist with an EC50 of 5.2 nM for human GPR120. 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 .
    AZ13581837
  • HY-133151
    CXCR6 antagonist 1

    		CXCR Cancer
    CXCR6 antagonist 1 (Compound 81) is an orally active CXCR6 antagonist. CXCR6 antagonist 1 inhibits the CXCR6 receptor signaling pathway, including β-arrestin recruitment and Forskolin (HY-15371)-induced cAMP production. CXCR6 antagonist 1 reduces tumor growth in a mouse xenograft model of hepatocellular carcinoma. CXCR6 antagonist 1 can be used in research related to hepatocellular carcinoma .
    CXCR6 antagonist 1
  • HY-19867
    Burixafor

    TG-0054

    		 CXCR Cancer
    Burixafor (TG-0054) is a potent CXCR4 antagonist with a pIC50 of 7.4. Burixafor 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 mobilizes CD34 + hematopoietic stem/progenitor cells (HSPC) from the bone marrow to the peripheral blood. Burixafor can be used for research on autologous hematopoietic stem cell transplantation (ASCT) .
    Burixafor

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