| Bioactivity | Carnostatine hydrochloride (SAN9812 hydrochloride) is a potent and selective carnosinase 1 (CN1) inhibitor with a Ki of 11 nM for human recombinant CN1. Carnostatine hydrochloride can be used for the treatment of diabetic nephropathy (DN)[1]. |
| Target | Ki: 11 nM (human CN1) |
| Invitro | 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 Km 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-naïve CN1-overexpressing mice[1]. Animal Model: |
| Name | Carnostatine hydrochloride |
| Formula | C10H17ClN4O4 |
| Molar Mass | 292.72 |
| Appearance | Oil |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |