Bioactivity | Carnostatine (SAN9812) is a potent and selective carnosinase 1 (CN1) inhibitor with a Ki of 11 nM for human recombinant CN1. Carnostatine (SAN9812) 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 |
Formula | C10H16N4O4 |
Molar Mass | 256.26 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |