Arrestin

ML339 a selective inhibitor of CXCR6(IC50 = 140 nM) with no response when screened against CXCR5 and CXCR4.

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.

Abaloparatide TFA (BIM 44058 TFA) is a parathyroid hormone-related protein (PTHrP) analog drug used to treat osteoporosis like the related drug teriparatide.

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.

TRV-120027 acetate is a β-arrestin-1-biased agonist of the angiotensin II receptor type 1 (AT1 receptor) and engages -arrestins while blocking G-protein signaling.

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.

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

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.

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

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

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.

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

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.

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.

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.

ELA-11 (human) acetate high affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

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.

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.

Abaloparatide (BA 058), a parathyroid hormone receptor 1 (PTHR1) analog and selective activator, promotes Gs cAMP signaling and β-arrestin recruitment, thereby enhancing bone formation and improving cortical structure in mice. This compound holds potential for osteoporosis research [1] [2].

Potent apelin (APJ) receptor agonist (Ki = 0.93 nM). Bioactive fragment of ELA-32. Activates Gαi1 pathway and β-arrestin-2 recruitment. Reduces arterial pressure in rat hearts. Active in vivo.

High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc

High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.

UNC9994 hydrochloride is a functionally selective, β-arrestin-biased dopamine D2 receptor (D2R) agonist (Ki: 79 nM) that selectively activates β-arrestin recruitment and signal transduction. UNC9994 hydrochloride is a Gi-regulated antagonist of cAMP production and a partial agonist of the D2R/β-arrestin-2 interaction, exhibiting psychostimulatory effects.

APJ receptor agonist 6 is a potent agonist of the APJ (apelin receptor) (Ki: 0.059 μM). (EC50: 6.22 μM).