Carnostatine (SAN9812) is a potent and selective carnosinase 1 ( CN1 ) inhibitor with a K i of 11 nM for human recombinant CN1. Carnostatine may be used to increase renal carnosine concentration as a potential therapeutic modality for diabetic nephropathy (DN). [1].

CN1 (human):ki： 11 nM

Carnostatine inhibits CN1 activity in human serum and serum of transgenic mice-overexpressing human CN1. At a carnosine concentration of 200 μM, Carnostatine has an IC 50 value of 18 nM on human recombinant CN1, i.e., close to the K m of 190 μM [1].

Subcutaneous administration of 30 mg/kg Carnostatine (SAN9812) results in a sustained reduction in circulating CN1 activity in human CN1 transgenic (TG) mice. Simultaneous administration of Carnosine and Carnostatine increases carnosine levels in plasma and kidney by up to 100-fold compared to treatment-na ve CN1-overexpressing mice [1]. Animal Model: Human carnosinase (CNDP1) transgenic mice on a BTBR wt/ob background [1] Dosage: 3 mg/kg i.v. or 30 mg/kg s.c. (Pharmacokinetic Analysis) Administration: Single bolus administration Result: Subcutaneous administration of 30 mg/kg led to a sustained reduction in circulating CN1 activity.