ZQ-16

• CAT Number: I011359
• CAS Number: 376616-73-8
• Molecular Formula: C10H16N2O2S
• Molecular Weight: 228.31
• Purity: ≥95%
• Synonyms: 2-hexylsulfanyl-4-hydroxy-1H-pyrimidin-6-one
• InChI: InChI=1S/C10H16N2O2S/c1-2-3-4-5-6-15-10-11-8(13)7-9(14)12-10/h7H,2-6H2,1H3,(H2,11,12,13,14)
• InChIKey: UYXOAKRMLQKLQX-UHFFFAOYSA-N
• SMILES: CCCCCCSC1=NC(=CC(=O)N1)O

ZQ-16 is a potent and selective GPR84 agonist with an EC50 value of 0.213 μM. ZQ-16 has no activity on the other free fatty acid receptors (FFARs), including GPR40, GPR41, GPR119 and GPR120[1].
ZQ-16 induces calcium response in a dose-dependent manner, with an EC50 value of 0.213 μM[1].
ZQ-16 also induces dose-dependent reduction of Forskolin-stimulated cAMP accumulation in HEK293 cells expressing GPR84 with an EC50 value of 0.134 μM[1].
ZQ-16 (10 μM; 5 min) also induces phosphorylation of ERK1/2 in GPR84-expressing HEK293 cells[1].
ZQ-16 induces GPR84 desensitization, internalization, and β-arrestin2 recruitment. ZQ-16 induced a dose-dependent recruitment of β-Arrestin2 towards GPR84 in HEK293 cells expressing both proteins with an EC50 value of 0.597 μM[1].

Reference

[1]. Qing Zhang, et al. Discovery and Characterization of a Novel Small-Molecule Agonist for Medium-Chain Free Fatty Acid Receptor G Protein-Coupled Receptor 84. J Pharmacol Exp Ther. 2016 May;357(2):337-44.
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