CID-16020046

CID-16020046 is a GPR55 inverse agonist that antagonizes GPR55 constitutive activity with an IC50 value of 15 µM. It inhibits GPR55-mediated ERK1/2 phosphorylation, LPI-induced Ca2+ signaling (IC50 = 0.21 µM in HEK-GPR55 cells), and GPR55-mediated transcription factor activation. It does not affect ERK1/2 phosphorylation or transcription factor activation in CB receptor expressing cells and demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptors. This compound has been shown to block GPR55-mediated endothelial wound healing and reverse LPI-inhibited platelet aggregation.Formal Name: 4-[4,6-dihydro-4-(3-hydroxyphenyl)-3-(4-methylphenyl)-6-oxopyrrolo[3,4-c]pyrazol-5(1H)-yl]-benzoic acid. CAS Number: 834903-43-4. Molecular Formula: C25H19N3O4. Formula Weight: 425.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml. lambdamax: 280 nm. SMILES: OC(C(C=C1)=CC=C1N2C(C3=CC=CC(O)=C3)C4=C(NN=C4C5=CC=C(C)C=C5)C2=O)=O. InChi Code: InChI=1S/C25H19N3O4/c1-14-5-7-15(8-6-14)21-20-22(27-26-21)24(30)28(18-11-9-16(10-12-18)25(31)32)23(20)17-3-2-4-19(29)13-17/h2-13,23,29H,1H3,(H,26,27)(H,31,32). InChi Key: VGUQVYZXABOXCX-UHFFFAOYSA-N.