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Description: MK-0354 is a novel and potent partial agonist of GPR109a receptor for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 uM, showed no activation of GPR109b. It can be potentially used for the treatment atherosclerosis. Treatment with MK-0354 for 7 days resulted in plasma FFA suppression with minimal cutaneous flushing. However, 4 weeks of treatment with MK-0354 failed to produce changes in high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, or triglycerides.
References: J. Med. Chem., 2008, 51 (16); J Clin Lipidol. 2008 Oct; 2(5):375-383.
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