GPR55 Antagonist

CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC₅₀ of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca²⁺ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.

ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC₅₀ of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats.

Tetrahydromagnolol (Magnolignan), the main metabolite of Magnolol, is a potent and selective cannabinoidCB2 receptor agonist (EC₅₀ =170 nM) and GPR55 antagonist. The K_i of Tetrahydromagnolol for CB2 is 416 nM, 20-fold higher than for the CB1 receptor. Magnolol shows antifungal, anti-inflammatory and analgesic effects.

ML191 (CID23612552) is a GPR55 antagonist. ML191 inhibits ERK phosphorylation and PKC β II translocation downstream of GPR55 signaling. ML191 suppresses LPI-induced activation of ERK1/2 and p38 MAPK signaling, blocks the transcription of RANKL-induced osteoclastogenesis markers, and reduces the bone resorption activity of mature osteoclasts promoted by RANKL. ML191 can be used to investigate diseases associated with bone degradation caused by excessive osteoclast activation, such as osteoporosis and bone damage during the formation stage of bone metastases.

ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation.

PSB-SB-487 is a potent GPR55 antagonist and CB₂ agonist with an IC₅₀ value of 0.113 µM for GPR55, and a K_i value of 0.292 µM for human CB₂. PSB-SB-487 can be used for researching diabetes, Parkinson’s disease, neuropathic pain, and cancer.

KLS-13019 is an orally active GPR55 receptor antagonist and a structural analogue of cannabidiol (CBD). It can prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rats.

Cyclic peptide P1-1 is a high-potent GPR55 antagonist. Cyclic peptide P1-1 antagonizes GPR55 and suppresses collagen secretion. Cyclic peptide P1-1 reduces ROS production, attenuates ER stress, and inhibits mitochondria-associated Apoptosis. Cyclic peptide P1-1 inhibits the expression of α-SMA and COL1α. Cyclic peptide P1-1 ameliorates CCl₄ (HY-Y0298)-induce and MCD-diet-induce acute liver inflammation and fibrosis.

CID 16020046 (Standard) is the analytical standard of CID 16020046. This product is intended for research and analytical applications. CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.