ML194 (CID9581011) is an antagonist of GPR35, a GPRC receptor expressed in nervous system tissue, in the GI tract particularly in pancreas and small intestine, followed by colon, spleen, and immune cells, and also expressed in gastric carcinomas. GPR35 is being investigated for potential therapeutic importance in a variety of areas including pain, hypertension, cancer, diabetes and asthma. ML194 is more membrane penetrant and more potent than earlier synthetic antagonists, with an IC50 of 160nM. ML194 was also found to rescue the cell-surface expression of mutant GPR35 receptors, likely acting as a pharmacological chaperone to alter the misfolded receptor structure.
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