化合物 T10684 T10684

Product Introduction
Bioactivity


英文名: Carnostatine

描述: Carnostatine (SAN9812) 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 可用于治疗糖尿病性肾病 (DN) 。

体外活性: Carnostatine inhibits CN1 activity in human serum and serum of transgenic mice-overexpressing human CN1. At a carnosine concentration of 200 μM, Carnostatine has an IC 50 value of 18 nM on human recombinant CN1, i.e., close to the K m of 190 μM [1].

体内活性: Subcutaneous administration of 30 mg/kg Carnostatine (SAN9812) results in 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] Dosage: 3 mg/kg i.v. or 30 mg/kg s.c. (Pharmacokinetic Analysis) Administration: Single bolus administration Result: Subcutaneous administration of 30 mg/kg led to a sustained reduction in circulating CN1 activity.

存储条件: keep away from moisturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: SAN-9812 | SAN 9812 | Carnostatine

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途