Search Result
Results for "
β-arrestin2
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-119706
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Barbadin
Maximum Cited Publications
16 Publications Verification
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Apoptosis
Arrestin
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Others
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Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis [2].
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- HY-138097
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Chemerin Receptor
Aldehyde Dehydrogenase (ALDH)
Cholinesterase (ChE)
Apoptosis
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Cancer
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α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity [2].
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- HY-14299
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research [2].
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- HY-145404
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Opioid Receptor
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Metabolic Disease
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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 [2].
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- HY-14299A
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QAB149
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research [2].
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- HY-P2106
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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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 .
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- HY-19867A
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TG-0054 hydrobromide
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CXCR
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Cardiovascular Disease
Cancer
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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) [2].
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- HY-P1102
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TC14012
4 Publications Verification
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CXCR
HIV
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Infection
Cancer
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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 [2].
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- HY-W010907
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GPR35
ERK
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Neurological Disease
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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 .
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- HY-169841
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5-HT Receptor
Arrestin
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Neurological Disease
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IHCH-7086 is a blood-brain barrier-permeable, partial β-arrestin-biased agonist of 5-HT2AR with a Ki of 12.59 nM. IHCH-7086 blocks D-lysergic acid diethylamide-induced head-twitch response in mice and alleviates depression-like behaviors in mice subjected to acute restraint stress or injected with Corticosterone (HY-B1618). IHCH-7086 is applicable to research related to depression [2].
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- HY-164795
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
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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 [2].
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- HY-164795A
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Neurotensin Receptor
Arrestin
iGluR
ERK
Sodium Channel
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Neurological Disease
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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 [2].
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- HY-119486A
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(Rac)-PF-06649751; (Rac)-CVL-751
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Dopamine Receptor
Arrestin
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Neurological Disease
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(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 .
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- HY-111385
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Dopamine Receptor
5-HT Receptor
Arrestin
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Neurological Disease
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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 .
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- HY-123813
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CXCR
Arrestin
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Cancer
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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 [2] .
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- HY-12557
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γ-Glu-Val
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Endogenous Metabolite
CaSR
Wnt
TNF Receptor
Interleukin Related
PPAR
β-catenin
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Inflammation/Immunology
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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 .
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- HY-117829
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UNC9994
2 Publications Verification
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Dopamine Receptor
5-HT Receptor
Histamine Receptor
Arrestin
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Neurological Disease
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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 Gi-regulated cAMP production. Antipsychotic Activity .
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- HY-100677
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CXCR
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Endocrinology
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VUF11207 (Compound 29) is a CXCR7 agonist and a high-potency CXCR7 (pKi of 8.1) ligand that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
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- HY-P2106A
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Apelin Receptor (APJ)
Arrestin
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Cardiovascular Disease
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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 .
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- HY-120920
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Dopamine Receptor
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Inflammation/Immunology
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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 .
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- HY-108656
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P2Y Receptor
Arrestin
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Cardiovascular Disease
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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 [2] .
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- HY-106481
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GPR35
Histamine Receptor
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Inflammation/Immunology
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Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide [2] .
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- HY-14299AR
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QAB149 (Standard)
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Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research [2].
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- HY-108656A
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P2Y Receptor
Arrestin
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Cardiovascular Disease
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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 [2] .
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- HY-163671
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GPR52
Arrestin
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Neurological Disease
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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 .
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- HY-110302
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-145278
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RXFP Receptor
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Neurological Disease
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RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC50=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC50 values in the range of 10-22 nM .
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- HY-14299R
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Reference Standards
Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Indacaterol (Standard) is the analytical standard of Indacaterol. This product is intended for research and analytical applications. Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research [2].
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- HY-175306
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EBI2/GPR183
Arrestin
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Inflammation/Immunology
Cancer
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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 .
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- HY-179226
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Molecular Glues
Adrenergic Receptor
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Inflammation/Immunology
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AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma .
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- HY-P3346
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Apelin Receptor (APJ)
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Cardiovascular Disease
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NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal) (compound 39) is a potent APJ agonist, with a Ki 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 .
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- HY-175366
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Opioid Receptor
Arrestin
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Neurological Disease
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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 .
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- HY-113689
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Cannabinoid Receptor
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Neurological Disease
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GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research .
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- HY-138951
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- HY-163277
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Opioid Receptor
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Inflammation/Immunology
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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 .
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- HY-P11246
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RXFP Receptor
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Metabolic Disease
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A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a Ki value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (Ki = 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 .
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- HY-179471
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GPR84
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Inflammation/Immunology
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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 .
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- HY-161717
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Adenosine Receptor
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Cardiovascular Disease
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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 .
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- HY-178203
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Cannabinoid Receptor
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Neurological Disease
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AM12814 is a potent and partial CB1 and CB2 agonist with Ki values of 0.7 nM and 3.4 nM. AM12814 can inhibit cAMP accumulation and recruitse β-arrestin 2. AM12814 exhibits cannabimimetic effects. AM12814 can be used for the research of neurological disease, suah as catalepsy .
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- HY-P1102A
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CXCR
HIV
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Infection
Cancer
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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 [2].
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- HY-144705
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Cannabinoid Receptor
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Neurological Disease
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GAT564 (Compound 15d) is a potent allosteric modulator of cannabinoid 1 receptor (CB1R) with EC50s of 87 and 320 nM respectively for cAMP and β-arrestin2. GAT564 markedly promotes orthosteric ligand binding to hCB1R. GAT564 is efficacious as a topical agent that significantly reduces intraocular pressure (IOP) in the ocular normotensive murine model of glaucoma .
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- HY-155184
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Adenosine Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
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A3AR agonist 2 (Compound 19) a selective A3AR agonist (Ki: 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.
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- HY-W664041
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Dopamine Receptor
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Neurological Disease
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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 .
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- HY-115615
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CXCR
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Endocrinology
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VUF11207 (Compound 29) TFA is a CXCR7 agonist (pKi of 8.1) that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7 .
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- HY-150057
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Cannabinoid Receptor
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Others
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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 .
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- HY-119234
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CXCR
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Inflammation/Immunology
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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 .
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- HY-155183
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Adenosine Receptor
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Inflammation/Immunology
Cancer
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A3AR agonist 1 (Compound 12) is an A3AR agonist (Ki: 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 .
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- HY-173052
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CXCR
CCR
Arrestin
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Inflammation/Immunology
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SLW131 is a CCR7 antagonist with a Ki value of 9.85 nM. SLW131 inhibits CCL19-induced Go protein activation with an IC50 of 29.4 μM, and suppresses β-arrestin2 recruitment with an IC50 of 6.0 μM. SLW131 serves as a probe for investigating the biological functions of CCR7 in cells. SLW131 is applicable to research related to rheumatoid arthritis .
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- HY-153162A
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Dopamine Receptor
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Neurological Disease
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(-)-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 .
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- HY-171069
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Free Fatty Acid Receptor
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Metabolic Disease
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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 .
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- HY-14299C
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Adrenergic Receptor
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Inflammation/Immunology
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Indacaterol xinafoate is an orally active long-acting β2-adrenergic agonist (LABA) with bronchodilatory effect. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol xinafoate can be utilized in asthma research [2].
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- HY-14299D
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
Cancer
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Indacaterol acetate is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol acetate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol acetate can also be used in cardiovascular disease research [2].
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- HY-116445
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Dopamine Receptor
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Neurological Disease
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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 .
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- HY-174466
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5-HT Receptor
Arrestin
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Neurological Disease
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5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 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 .
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- HY-47412
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Dopamine Receptor
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Neurological Disease
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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 .
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- HY-165453
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Histamine Receptor
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Inflammation/Immunology
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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 .
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-
- HY-183777
-
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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 .
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- HY-19867
-
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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) [2].
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- HY-181822
-
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Formyl Peptide Receptor (FPR)
Arrestin
PKA
Interleukin Related
|
Cardiovascular Disease
|
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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 .
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- HY-179606
-
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Transmembrane Glycoprotein
Arrestin
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
RWT9996 is a balanced GPR17 antagonist. RWT9996 has an inhibitory effect on G protein activation and β-arrestin-2 recruitment induced by MDL-29951. RWT9996 inhibits the phosphorylation of ERK/CREB and the accumulation of inositol phosphate (b IP1) induced by MDL-29951. RWT9996 can be used for the study of neurological diseases .
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- HY-181102
-
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G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
Inflammation/Immunology
|
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TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes .
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- HY-W399025
-
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Opioid Receptor
Arrestin
|
Neurological Disease
|
|
ID110460001 is a full agonist of μ-opioid receptor and an agonist of δ-opioid receptor. ID110460001 exhibits high intrinsic efficacy for G protein pathway activation of μ-opioid receptor, and this property is not affected by the reduction in receptor quantity. ID110460001 acts only as a very weak partial agonist in the β-arrestin-2 pathway of both receptors, and binds to μ-opioid receptor via a specific mode. The efficacy of ID110460001 in the G protein pathway of δ-opioid receptor is sensitive to changes in receptor quantity. ID110460001 can be used in pain-related research .
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-
- HY-W414109
-
|
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Opioid Receptor
Arrestin
|
Neurological Disease
|
|
ID110460002 possesses both full agonist activity at the μ-opioid receptor (OPRM) and agonist activity at the δ-opioid receptor (OPRD). ID110460002 acts as a potent agonist for the G protein pathways of both receptors, but exhibits only very weak partial agonist activity towards the β-arrestin-2 pathway. The agonistic potency of ID110460002 at OPRM has extremely high intrinsic activity and is unaffected by reduced receptor expression levels, while its potency at OPRD depends on receptor expression levels. ID110460002 displays tissue- or organ-dependent properties, and serves as a critical compound for investigating pain mechanisms and analgesia .
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-
- HY-179705
-
|
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Opioid Receptor
|
Neurological Disease
|
|
MOR agonist-5 is a selective and potent mu-opioid receptor (MOR) agonist with an EC50 of 0.25 nM. MOR agonist-5 shows an EC50 of 10 nM for DOR and >10000 nM for KOR and NOR. MOR agonist-5 exerts significant antinociceptive activity. MOR agonist-5 can be used for the research of pain .
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-
- HY-123813A
-
|
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CXCR
Arrestin
|
Cancer
|
|
CCX-777 formic is an orthosteric binder and partial agonist of CXCR7/ACKR3. CCX-777 formic induces the recruitment of β-arrestin 2 and affects the rebinding of chemokines to ACKR3. CCX-777 formic functions to stabilize the ACKR3 receptor and promotes the formation of a monodisperse, stable complex of the receptor in DDM/CHS micelles. CCX-777 formic is widely used in cancer-related research [2] .
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-
- HY-180845
-
|
|
G protein-coupled Bile Acid Receptor 1
|
Metabolic Disease
|
|
TGR5 agonist 9 is a highly selective and orally active TGR5 allosteric agonist with EC₅₀ values for hTGR5 and mTGR5 of 0.48 and 0.49 μM, respectively. TGR5 agonist 9 can recruit β-arrestin 1 (EC₅₀ = 78.8 μM) and β-arrestin 2 (EC₅₀ = 12.3 μM), and has a higher efficacy in cAMP accumulation (EC₅₀ = 0.48 μM). TGR5 agonist 9 exhibits a significant hypoglycemic effect in the ICR mouse model. TGR5 agonist 9 can be used for research on diabetes .
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-
- HY-185356
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
SR-14968 is a full, allosteric and non-competitive MOR agonist, with an EC50 of 88 nM for MOR in mouse brainstem. SR-14968 stabilizes MOR in a G protein signaling state that is resistant to washout but reversible by antagonists. SR-14968 induces respiratory depression in mice. SR-14968 can be used in pain-related research .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2106
-
|
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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 .
|
-
- 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 [2].
|
-
- HY-12557
-
|
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 .
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-
- HY-P2106A
-
|
|
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 .
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-
- HY-138951
-
-
- HY-P11246
-
|
|
RXFP Receptor
|
Metabolic Disease
|
|
A13:B7-24-GG is an engineered analogue of insulin-like peptide 5 (INSL5), a selective RXFP4 agonist with a Ki value of 2.29 nM. A13:B7-24-GG has an extremely low binding affinity for RXFP3 (Ki = 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-P1102A
-
|
|
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 [2].
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