JBSNF-000088 is an inhibitor of nicotinamide N-methyltransferase (NNMT; IC50s = 1.8, 2.8, and 5 µM for human, monkey, and mouse NNMT, respectively).1 It inhibits NNMT and reduces 1-methyl-nicotinamide (MNA) levels in U2OS and 3T3L1 cells (IC50s = 1.6 and 6.3 µM, respectively). JBSNF-000088 (50 mg/kg) reduces visceral white adipose tissue (WAT) MNA levels, body weight, fed blood glucose levels, and plasma and liver triglyceride levels, and improves oral glucose tolerance in a mouse model of diet-induced obesity (DIO). It also improves glucose tolerance, without affecting body weight, in the ob/ob and db/db mouse models of insulin resistance and diabetes, respectively.

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