Carnostatine (SAN9812)
目录号 : GC34336
Carnostatine(SAN9812)是一种特异性和高选择性的肌肽酶(CN1)抑制剂，Ki为11nM。
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| Cas No. | SDF | ||
| Canonical SMILES | OC([C@@H](NC([C@@H](O)CCN)=O)CC1=CNC=N1)=O | ||
| 分子式 | C10H16N4O4 | 分子量 | 256.26 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.9023 mL | 19.5114 mL | 39.0229 mL |
| 5 mM | 0.7805 mL | 3.9023 mL | 7.8046 mL |
| 10 mM | 0.3902 mL | 1.9511 mL | 3.9023 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.PMID:29922921DOI:10.1007/s00726-018-2601-z
Carnosinase 1 (CN1) has been postulated to be a susceptibility factor for developing diabetic nephropathy (DN). Although its major substrate, carnosine, is beneficial in rodent models of DN, translation of these findings to humans has been hampered by high CN1 activity in human serum resulting in rapid degradation of carnosine. To overcome this hurdle, we screened a protease-directed small-molecule library for inhibitors of human recombinant CN1. We identified SAN9812 as a potent and highly selective inhibitor of CN1 activity with a Ki of 11 nM. It also inhibited CN1 activity in human serum and serum of transgenic mice-overexpressing human CN1. Subcutaneous administration of 30 mg/kg SAN9812 led to a sustained reduction in circulating CN1 activity in human CN1 transgenic (TG) mice. Simultaneous administration of carnosine and SAN9812 increased carnosine levels in plasma and kidney by up to 100-fold compared to treatment-naïve CN1-overexpressing mice. To our knowledge, this is the first study reporting on a potent and selective CN1 inhibitor with in vivo activity. SAN9812, also called carnostatine, may be used to increase renal carnosine concentration as a potential therapeutic modality for renal diseases linked to glycoxidative conditions.