Carnostatine hydrochloride (SAN9812 hydrochloride) 是一种有效的选择性肌肽酶 1 (CN1) 抑制剂，对人重组 CN1 的 Ki 值为 11 nM。Carnostatine hydrochloride 可用于治疗糖尿病性肾病 (DN)。
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-na?ve CN1-overexpressing mice[1]. Animal Model: Human carnosinase (CNDP1) transgenic mice on a BTBR wt/ob background[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. 2019 Jan;51(1):7-16.
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