Arrestin Activator

AT1R-agonist-1 is an angiotensin II type 1 receptor (AT1R) agonist with a K_i value of 1.4 nM. AT1R-agonist-1 exhibits low Gαq activity, retains β-arrestin recruitment function, and accesses the deep allosteric pocket inside AT1R via its flexible side chain. AT1R-agonist-1 possesses positive inotropic effects (enhancing cardiac contractile function) and causes almost no increase in blood pressure. AT1R-agonist-1 can be used for research on conditions such as refractory cardiogenic shock.

3-ethoxy-5,6-dibromosalicylaldehyde is a potent, non-competitive, selective IRE1 (including IRE1α) inhibitor (IC₅₀s: ∼0.12 μM for hIRE1α-cyto; 6 μM for yeast Ire1). 3-ethoxy-5,6-dibromosalicylaldehyde inhibits XBP-1 splicing. 3-ethoxy-5,6-dibromosalicylaldehyde induces Apoptosis. 3-ethoxy-5,6-dibromosalicylaldehyde upregulates the mRNA expression level of TXNIP, while downregulating the expression level of TXN. 3-ethoxy-5,6-dibromosalicylaldehyde exhibits anticancer activity against pancreatic cancer. 3-ethoxy-5,6-dibromosalicylaldehyde significantly inhibits chikungunya virus replication.

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 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.

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.

Elabela(19-32) is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) activates the G_αi1 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) TFA is an active fragment of ELABELA (ELA) that binds to apelin receptor (APJ). Elabela(19-32) TFA activates the G_αi1 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.

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.

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.

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.

NCGC00135472 is a potent agonist of resolvin D1 receptor (DRV1), with the EC₅₀ of 0.37 nM and 0.05 μM for β-arrestin and cAMP activities, respectively.

MRS542 is a nucleoside A3 AR antagonist with a pK_i of 8.74. MRS542 also acts as a partial agonist (pEC₅₀ = 7.76) in promoting β-arrestin translocation. MRS542 can be converted into an agonist by LUF6000 (HY-13236). MRS542 can be used for cardiovascular disease research.

ISAM-CG557 is a selective CB2R agonist, with a K_i of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC₅₀s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.

ML138 is a blood-brain barrier-permeable κ-opioid receptor (KOR) agonist, with an EC₅₀ value of 0.87 μM and a human K_i value of 2.4 nM for human receptors; it exhibits high selectivity for KOR over μ, δ and other receptors. ML138 activates β-arrestin (beta-arrestin)-mediated signaling pathways, stimulates G protein coupling, and activates the downstream extracellular regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAP kinase) signaling pathway. ML138 is applicable to research related to addictive behaviors.

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.