Carnostatine hydrochloride

• CAT Number: I046019
• Molecular Formula: C10H17ClN4O4
• Molecular Weight: 292.72
• Purity: ≥95%
• Synonyms: (2S)-2-[[(2S)-4-amino-2-hydroxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoic acid;hydrochloride
• InChI: InChI=1S/C10H16N4O4.ClH/c11-2-1-8(15)9(16)14-7(10(17)18)3-6-4-12-5-13-6;/h4-5,7-8,15H,1-3,11H2,(H,12,13)(H,14,16)(H,17,18);1H/t7-,8-;/m0./s1
• InChIKey: DVOGVAYBGHFTIP-WSZWBAFRSA-N
• SMILES: C1=C(NC=N1)CC(C(=O)O)NC(=O)C(CCN)O.Cl

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].
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].
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].

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.
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