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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
β-arrestin-1
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "β-arrestin-1" in MCE Product Catalog:
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20 Publications Verification
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 [1] .
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3 Cited Publications
Cat. No.: HY-P2141A
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Cat. No.: HY-178323
CAS No.: 3048608-87-0
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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].
Cat. No.: HY-136960
CAS No.: 2135743-21-2
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β2AR antagonist 1 is a potent β2-adrenergic receptor (β2AR) inhibitor. β2AR antagonist 1 exhibits high selectivity for β2AR over β1AR, vasopressin receptor type 2, and angiotensin type 1 receptor. β2AR antagonist 1 stabilizes the inactive conformation of β2AR and interferes with its coupling to G proteins and β-arrestins .
Cat. No.: HY-162728
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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 [1].
Cat. No.: HY-155099
CAS No.: 3033813-47-4
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FGH31 (Compound 24) is a potent, selective, GRK2 dependency dopamine D4 agonist, with the Ki of 1.6 nM. FGH31 partial activates β- arrestin .
Cat. No.: HY-187689
CAS No.: 1005056-10-9
RKN5755 is a β-arrestin1 inhibitor and a selective inhibitor of activated fibroblasts. RKN5755 binds to β-arrestin1 and interferes with the cofilin signaling pathway mediated by this protein to block its function. RKN5755 not only inhibits the enhanced migratory effect of fibroblasts co-cultured with cancer cells, but also prevents the inhibitory effect of EP3 agonists on the EP2 receptor-induced elevation of tetrodotoxin-resistant sodium currents in mouse dorsal root ganglion neurons. RKN5755 is widely used in research on related diseases such as cancer metastasis and pain [1] .
Cat. No.: HY-183777
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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 [1].
Cat. No.: HY-P810789
Synonyms: ARR1, ARRB1, Beta-arrestin-1, arrestin beta-1, Non-visual arrestin-2
Cat. No.: HY-181822
CAS No.: 2375684-52-7
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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 [1].
Cat. No.: HY-P80569A
Synonyms: ARB1; ARR1; ARRB1; ARRB1_HUMAN; arrestin 2; arrestin beta 1; arrestin beta-1; Beta-arrestin-1.
Cat. No.: HY-120093
CAS No.: 1663564-42-8
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GAT100 is a negative allosteric modulator and covalent allosteric probe for cannabinoid receptor type 1 (CB1R). GAT100 acts as a positive allosteric modulator for orthosteric agonist CP55,940 binding to regulate the CB1R signaling pathway. GAT100 reduces the potency and efficacy of orthosteric CB1R agonists in terms of β-arrestin 1 recruitment, phosphorylation of PLCβ3 and ERK1/2, cAMP accumulation, and CB1R internalization. GAT100 is applicable to the research of psychobehavioral and somatic diseases [1] .
Cat. No.: HY-180845
CAS No.: 2931879-67-1
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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 [1].
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
