Carnostatine(SAN9812)是一种特异性和高选择性的肌肽酶(CN1)抑制剂，Ki为11nM。
Carnostatine (SAN9812) is a specific and highly selective carnosinase (CN1) inhibitor with a Ki of 11 nM.
Carnostatine (SAN9812) is a potent CN1 activity inhibitor 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. Carnostatine is a competitive inhibitor, showing a right-shift in its IC50 value with increasing carnosine concentration. The Ki value of Carnostatine is determined as 11 nM[1].
CN1 activity is measured after a single subcutaneous bolus of 30 mg/kg Carnostatine (SAN9812). Animals are stratified according to their baseline serum carnosinase activity into a high-activity- (> 250 µmol/mL/h) and a low-activity ( 8 h. At the last sampling time point 16 h after Carnostatine administration, serum carnosinase activity is still reduced by 40% in the low-activity group and by 75% in the high-activity group[1].
[1]. Qiu J, et al. Identification and characterisation of carnostatine (SAN9812), a potent and selective carnosinase (CN1) inhibitor with in vivo activity. Amino Acids. 2018 Jun 20.
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