Carnostatine

Carnostatine (SAN9812) is a potent and selective carnosinase 1 (CN1) inhibitor with a K_i of 11 nM for human recombinant CN1. Carnostatine (SAN9812) can be used for the treatment of diabetic nephropathy (DN)^[1]. IC50 & Target:Ki: 11 nM (human CN1)^[1] In Vitro: Carnostatine (SAN9812) also inhibits CN1 activity in human serum and serum of transgenic mice-overexpressing human CN1. Carnostatine, with an IC₅₀ value of 18 nM on human recombinant CN1 at a carnosine concentration of 200 μM, i.e., close to the K_m of 190 μM^[1]. In Vivo: Subcutaneous administration of 30 mg/kg Carnostatine (SAN9812) leads to 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].