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.

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.

GAT211 (AZ-4) is a selective and potent cannabinoid 1 receptor (CB1R) orthosteric modulator (PAM) with high affinity for cAMP and β-arrestin2.GAT211 has IOP-lowering and antipsychotic effects and can be used in the study of epilepsy.

ML417 is a selective and brain-penetrant agonist of D3 dopamine (EC50: 38 nM).

Arrestin-3 modulator-1 (Compound LSH-3) is a regulator of Arrestin-3. It binds with Arrestin-3 at the inter-domain interface. This compound enhances the recruitment of Arrestin-3 to phosphorylated-deficient β2AR in cells and elevates FRET levels. Arrestin-3 modulator-1 is applicable in studies related to congenital diseases such as retinal degeneration, hyperthyroidism, and obesity.

CID 2745687 is a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50 = 6.70. CID 2745687 cannot effectively antagonize the agonist effects of either Zaprinast or Cromolyn disodium at rodent ortholog of GPR35 in vitro[1]. However, CID 2745687 can reverse lodoxamide-mediated anti-fibrotic effects in mice in vivo[2].

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

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

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.

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.

CB1R Allosteric modulator 3 is a potent CB1R modulator that inhibits cAMP and β-Arrestin and can be used for the study of obesity and nicotine addiction.

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.

TC14012 acetate is a serum-stable derivative of T140 which is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is also a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-cancer activity and anti-HIV activity.

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.

SCH-900875 is an orally active, brain-penetrant, and selective inhibitor of the CXCR3 receptor, demonstrating significant selectivity towards CXCR1 and CXCR2 receptors as well. By binding to CXCR3, SCH-900875 blocks the ligands CXCL9, CXCL10, and CXCL11, thereby inhibiting downstream G protein and β-arrestin signaling pathways and reducing inflammation cell migration. This compound holds potential for research into autoimmune diseases (such as rheumatoid arthritis and multiple sclerosis) and inflammatory conditions (such as psoriasis and inflammatory bowel disease).

CT-996 is an orally active GLP-1 receptor agonist that exhibits preferential cAMP signaling and reduces endocytosis. Oral administration of CT-996 improves glycemic control and reduces body weight and body fat.

D1R antagonist 2 (Compound 13a) is a blood-brain barrier-permeable D1R antagonist, with IC50 values of 35.6 nM for cAMP-based D1R and 70 nM for β-arrestin-based D1R. It effectively inhibits D1R-mediated cAMP and β-arrestin recruitment and is applicable in studies of neurodegenerative and neuropsychiatric disorders, such as schizophrenia, Parkinson's disease, and Alzheimer's disease.

ISAM-CG557 is a selective CB2R agonist with a Ki of 54.6 nM. It reduces intracellular ROS levels and caspase activity, demonstrating significant MAPK bias and moderate G-protein bias, with CB2REC50 values of 0.60 nM for cAMP, 60.9 nM for β-arrestin, and 0.03 nM for MAPK. ISAM-CG557 exerts potent anti-inflammatory effects by decreasing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. It is utilized in the study of neuroinflammation and neurodegenerative diseases.

RWT9996 acts as a balanced GPR17 antagonist. It inhibits G protein activation and β-arrestin-2 recruitment induced by MDL-29951. Additionally, RWT9996 suppresses MDL-29951-induced ERK/CREB phosphorylation and inositol phosphate (IP1) accumulation. This compound is useful for researching neurological disorders.

CCX-777 formic is a partial agonist that recruits β-arrestin-2 to ACKR3 (atypical chemokine receptor 3). It has applications in cancer research.

CCX777 is a partial agonist recruited to ACKR3 by β-arrestin-2 and is used in cancer research.

UNC9994 is a β-arrestin-biased dopamine D₂ receptor agonist (β-arrestin EC50 = 50 nM; Emax = 97%) with robust in vivo antipsychotic drug-like activities.

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

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.