Arrestin Inhibitor

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.

RWT9996 is a GPR17 antagonist. RWT9996 inhibits GPR17-mediated signal transduction processes, including G protein activation and β-arrestin-2 recruitment. RWT9996 inhibits MDL-29951 (HY-16312)-mediated phosphorylation of ERK1/2, phosphorylation of CREB, and accumulation of inositol phosphate (IP1) in oligodendrocyte precursor cells in vitro. RWT9996 can be used in studies related to demyelinating diseases.

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.

APJ receptor agonist 6 (compound 9) is a potent APJ (apelin receptor) agonist, with K_i of 1.3 μM. APJ receptor agonist 6 has EC₅₀ values of 0.070 , 0.097, and 0.063 μM for calcium, cAMP, and β-arrestin, respectively.

ADX68692 is an orally active FSHR negative allosteric regulator, with an IC₅₀ value of 140 nM against hFSHR. ADX68692 antagonizes hCG (HY-107953)-mediated cAMP production, β-arrestin 2 recruitment, and the LH/CGR signaling pathway. ADX68692 partially inhibits testosterone synthesis. ADX68692 blocks follicle growth, disrupts the estrous cycle in rats, and reduces the pregnancy rate in rats. ADX68692 can be used in research related to contraception and endometriosis.

CB1R Allosteric modulator 3 is a CB1R positive allosteric modulator. CB1R Allosteric modulator 3 has potent inhibition of cAMP and β-Arrestin with EC₅₀ values of 0.018 μM and 1.241 μM, respectively.

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].

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.

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.

SLW131 is a CCR7 antagonist with a K_i 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.

SKL1223 is an orally effective thioredoxin-interacting protein (TXNIP) inhibitor with an IC₅₀ of 0.64 µM. SKL1223 interacts with the E-box region of the TXNIP promoter to inhibit TXNIP transcription and related signaling pathways. SKL1223 reduces hepatic glucose output. SKL1223 exerts hypoglycemic effects by regulating the action of glucagon, and modulates blood glucose levels in Streptozotocin (HY-13753)-induced and obesity-induced diabetic mice. SKL1223 can be used in the research of type 1 diabetes and type 2 diabetes.

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.

W2476 is a regulator of thioredocin-interacting protein signaling pathway. W2476 promotes competitive binding of forkhead box O1 transcription factor (FOXO1). W2476 can ameliorate β-cell dysfunction and enhance insulin secretion in diabetic mouse model.

ML221 (Standard) is the analytical standard of ML221 (HY-103254). This product is intended for research and analytical applications. ML221 is a potent apelin (APJ) functional antagonist, inhibiting apelin-13-mediated activation of APJ, with IC₅₀s of 0.70 μM in the cAMP assay, and 1.75 μM in the β-arrestin assay, and EC80 of 10 nM in both assays.

Forsythoside I (Standard) is the analytical standard of Forsythoside I (HY-N5042). This product is intended for research and analytical applications. Forsythoside I is an orally active caffeoyl phenylethanoid glycoside (CPG) that can be isolated from Forsythia suspense (Thunb.) Vahl. Forsythoside I has anti-inflammatory activity and can exert a protective effect in a mouse model of acute lung injury.