β-arrestin

GPR35 agonist 3 is a synthetic GPR35 agonist with an EC50 value of 1.4 μg in the β-arrestin recruitment assay.GPR35 agonist 3 is used in the study of cancer, type 2 diabetes, and cardiovascular disease.

7-FluorotryptaMine HCl is a potent aromatic monoamine GPRC5A agonist that induces GPRC5A-mediated β-arrestin recruitment.7-FluorotryptaMine HCl can be used to study signalling pathways related to immunity and cancer.

GPR35 agonist 2 (TC-G 1001) is a potent GPR35 agonist.The EC50 values of GPR35 agonist 2 in the β-arrestin and Ca2+ release assays were 26 and 3.2 nM, respectively.

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1 GPR32 receptor in beta-blocker and cAMP assays with EC50s of 0.37 uM and 0.05 uM, respectively.NCGC00135472 induces in cells overexpressing recombinant DRV1 rapid impedance changes that stimulate phagocytosis of serum-treated zymoglycans.

GP 1a is a potent agonist of cannabinoid receptor 2 (CB2) (EC50=7.1), as shown in cAMP, GTPγS and β-arrestin recruitment assays. GP 1a is approximately 30-fold more selective for CB2 receptors than CB1 receptors and increases P-ERK1 2 expression in HL-60 cells in vitro. GP 1a is beneficial for skin wound healing. GP 1a inhibits inflammation and fibrogenesis while promoting epithelial re-formation.

Barbadin is a novel and specific inhibitor of β-arrestin β2-adaptin interaction with an IC50 value of 19.1 μM for β-arestin1 and 15.6 μM for β-arestin2. Barbadin potentiates the long term effects of lorcaserin on POMC neurons and weight loss. Barbadin potentiates the long-term effects of lorcaserin on POMC neurons and weight loss, blocks agonist-promoted endocytosis of prototypic β2-adrenergic, V2-vasopressin, and angiotensin-II-1 receptors, and may be useful in the study of obesity.

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.

MLS1547 (MLS000051547) is a highly efficacious agonist of G protein-biased dopamine D2 receptor with a Ki of 1.2 μM. MLS1547 stimulates D2R G protein-mediated signaling with EC50 of 0.37 μM in a calcium mobilization assay.

ML192 (CID1434953) is a selective GPR55 ligand antagonist. ML192 is an inhibitor that inhibits β-arrestin transport, ERK1 2 phosphorylation, and PKCβII translocation.

ELA-14(human) acetate is a fragment of ELA that binds to APJ, activates the Gαi1 and β-arrestin-2 signaling pathways, and induces receptor internalization similarly to its parent endogenous peptide.

TRV120027 TFA is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1R) and engages ß-arrestins while blocking G-protein signaling.

CYT-1010 is an mu-opioid receptor agonist. The EC50 for the inhibition of β-arrestin recruitment and cAMP production is 13.1 nM and 0.0053 nM, respectively.

CYT-1010 hydrochloride is an mu-opioid receptor agonist. The EC50 for β-arrestin recruitment and cAMP production inhibition were 13.1 nM and 0.0053 nM, respectively.

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of eumelanin, as well as acting as a moderate potency agonist of GPR35. In the U2OS cell line, DHICA demonstrates the ability to induce β-arrestin translocation signaling with an EC50 value of 23.2 μM. Additionally, it plays a significant role in promoting and protecting against DNA damage.

UNC10099984A (Compound 6) is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 of 6.2 nM for β-arrestin. This compound is useful for research into central nervous system diseases related to the D2 receptor.

KOR agonist 3 (Compound 5) is an agonist of the κ opioid receptor (κOR) with an EC50 of 0.88 nM. It also exhibits some activation of μOR, with an EC50 of 720 nM. However, KOR agonist 3 does not activate δOR at concentrations below 1 μM. Its ability to recruit β-Arrestin-2 is lower than that of U50488.

Fluorphine, an analog of Brorphine, binds to the μ-opioid receptor (MOR) with a Ki of 12.5 nM. It exhibits GTPγS binding activity with an EC50 of 75 nM and β-arrestin 2 recruitment activity with an EC50 of 377 nM, and it also has respiratory depressive effects.

SBI-810 is a functional selective β-arrestin-biased allosteric modulator of the neurotensin receptor 1 (NTSR1). In the presence of the endogenous ligand neurotensin (NT), SBI-810 regulates NTSR1 signaling through a G protein-specific mechanism. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, allowing NTSR1 to activate GoA and G12.

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERα (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote β-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 μM, 6.4 μM, and 1.7 μM, respectively.

SBI-810 hydrochloride is a functional selective allosteric modulator of the β-arrestin-biased neurotensin receptor 1 (NTSR1). It modulates NTSR1-G protein signaling in a G protein-specific manner in the presence of the endogenous ligand neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced Gq activation, partially antagonizes NT-induced Gi1 activation, while allowing activation of GoA and G12 by NTSR1.

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4, with an IC50 of 1.1 nM. This compound inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 of 0.9 nM. In RAW 264.7 macrophages, it reduces the expression of PGE2-induced IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C motif) ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase 1 (Arg1) mRNA. In the CT26 mouse colon cancer model, EP4 receptor antagonist 7, combined with an anti-PD-1 antibody, inhibits tumor growth and enhances CD8+ T cell infiltration into the tumor.

FFA2 agonist-1 (Compound 4) is an agonist of the free fatty acid receptor 2 (FFA2 GPR43) with an EC50 of 81 nM. It demonstrates activity in β-arrestin-2 recruitment and cAMP inhibition assays, with EC50 values of 1.2 μM and 0.53 μM, respectively. FFA2 agonist-1 can induce the mucosal response of appetite-regulating peptide YY (PYY), inhibit fat accumulation, and affect intestinal function and food intake, making it useful for obesity research.