ML-193 is a potent antagonist of GPR55 (IC₅₀ = 221 nM).^1,2 It displays selectivity for GPR55 over CB₁, CB₂, and GPR35. ML-193 inhibits GPR55-dependent ERK phosphorylation (IC₅₀ = 65 nM) and blocks translocation of PKCβII.¹ ML-193 blocks increases in intracellular calcium levels induced by lysophosphatidylinositol (LPI) in dissociated rat periaqueductal gray neurons and modulates pain perception in LPI-treated rats.³

≥98%

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CID-1261822;

1.Heynen-Genel, S.,Dahl, R.,Shi, S., et al. Screening for selective ligands for GPR55 – antagonists. NIH Mol.Libraries (2010).

2.Kotsikorou, E.,Sharir, H.,Shore, D.M., et al. Identification of the GPR55 antagonist binding site using a novel set of high-potency GPR55 selective ligands. Biochemistry 52(52), 9456-9469 (2013).

3.Deliu, E.,Sperow, M.,Console-Bram, L., et al. The lysophosphatidylinositol receptor GPR55 modulates pain perception in the periaqueductal gray. Mol.Pharmacol. 88(2), 265-272 (2015).