| Description | 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]. |
| In vitro | 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]. |
| In vivo | 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. |
| Target activity | CN1 (human):ki： 11 nM |
| Synonyms | SAN9812 |
| molecular weight | 256.26 |
| Molecular formula | C10H16N4O4 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Qiu J, et al. Identification and characterisation of carnostatine (SAN9812), a potent and selective carnosinase (CN1) inhibitor with in vivo activity. Amino Acids. 2019 Jan;51(1):7-16. |