β-arrestin2

Indacaterol (Onbrez; Arcapta) is a β2-Adrenergic Agonist. The mechanism of action of indacaterol is as an Adrenergic beta2-Agonist.

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.

Indacaterol maleate (QAB149) is an ultra-long-acting β-adrenoceptor agonist.

VUF11207 fumarate is an agonist of CXCR7 and a high-potency ligand of CXCR7 (pKi: 8.1).

VUF14480 is a covalent partial agonist that interacts with cysteine 98(3.36) of the human histamine H₄ receptor. VUF14480 was shown to be a partial agonist of hH4 receptor-mediated G protein signalling and β-arrestin2 recruitment. VUF14480 bound covalently to the hH₄ receptor with submicromolar affinity. Serine substitution of C98(3.36) prevented this covalent interaction.

58-G3 is an agonist of methuselah (Mth)-specific that acts by inducing dose-dependent calcium elevation and membrane translocation of β-arrestin2.

A3AR Agonist 1 (Compound 12), with a Ki of 25.8 nM, is a potent A3 adenosine receptor (A3AR) agonist that promotes β-arrestin2 recruitment with an effective concentration (EC50) of 5.17 nM. It serves as a research tool in various pathological conditions, including inflammatory diseases, ischemia, cancer, neuropathic pain, and liver diseases [1].

Compound 19, a selective A3 Adenosine Receptor (A3AR) agonist (K i : 22.1 nM), effectively stimulates β-arrestin2 recruitment with an EC 50 value of 4.36 nM. This compound is utilized in research pertaining to inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions [1].

(–)-IHCH7041 is a optical rotation negative isomer of IHCH7041. (–)-IHCH7041 is a DRD2 partial agonist. (–)-IHCH7041 showed EC50 = 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment. (–)-IHCH7041 exhibited a inhibition constant (Ki) of 22.44 nM binding affinity at DRD2. (–)-IHCH7041 has antidepressant properties and reverses cognitive impairment.

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

TC14012 TFA, a serum-stable derivative of T140, is a selective peptidomimetic CXCR4 antagonist with an IC50 value of 19.3 nM and also functions as a potent CXCR7 agonist, exhibiting an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. This compound demonstrates anti-HIV and anti-cancer activities [1] [2].

GAT564 (Compound 15d) is a highly effective allosteric modulator of the cannabinoid 1 receptor (CB1R), with EC50 values of 87 nM for cAMP and 320 nM for β-arrestin2. It significantly enhances the binding of orthosteric ligands to hCB1R and exhibits remarkable efficacy as a topical agent, significantly reducing intraocular pressure (IOP) in an ocular normotensive murine model of glaucoma [1].

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.

MRS5663 (Compound 3a), an A3AR agonist, exhibits an EC50 value of 5.62 nM in β-arrestin2 recruitment assays. This compound demonstrates cytoprotective effects in skeletal muscle ischemia-reperfusion injury claudication models.