Carnostatine(SAN9812)鏄竴绉嶇壒寮傛€у拰楂橀€夋嫨鎬х殑鑲岃偨閰?CN1)鎶戝埗鍓傦紝Ki涓?1nM銆侟br>璐у彿:ajcx13394
CAS:N/A
鍒嗗瓙寮廁C10H16N4O4
鍒嗗瓙閲忥細256.26
婧惰В搴?Soluble in DMSO
绾害锛?8%
瀛樺偍锛歋tore at -20掳C
搴撳瓨锛欬span> 鐜拌揣

Background:

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 ?M, i.e., close to the Km of 190 ?M. 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 ?mol/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.