MLN-4760
(Synonyms: GL-1001) 目录号 : GC31354
An ACE2 inhibitor
Cas No.:305335-31-3
Sample solution is provided at 25 µL, 10mM.
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MLN4760 is an inhibitor of angiotensin-converting enzyme 2 (ACE2; IC50 = 0.44 nM).1 It is selective for ACE2 over ACE and carboxypeptidase A (CPDA; IC50s = >100 and 27 ?M, respectively). MLN4760 inhibits ACE2 hydrolysis of angiotensin I in vitro when used at a concentration of 1 ?M.2 It also inhibits the protein-protein interaction between ACE2 and the severe acute respiratory coronavirus 2 (SARS-CoV-2) spike glycoprotein, also known as the surface glycoprotein.3 In vivo, MLN4760 inhibits exogenous recombinant ACE2-induced prevention of angiotensin II-induced hypertension in mice.2
1.Dales, N.A., Gould, A.E., Brown, J.A., et al.Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitorsJ. Am. Chem. Soc.124(40)11852-11853(2002) 2.Ye, M., Wysocki, J., Gonzalez-Pacheco, F.R., et al.Murine recombinant ACE2: Effect on angiotensin II-dependent hypertension and distinctive ACE2 inhibitor characteristics on rodent and human ACE2Hypertension60(3)730-740(2012) 3.Williams-Noonan, B.J., Todorova, N., Kulkarni, K., et al.An active site inhibitor induces conformational penalties for ACE2 recognition by the spike protein of SARS-CoV-2J. Phys. Chem. B125(10)2533-2550(2021)
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Animal experiment: |
Rats[3]In a related experiment to evaluate the role of central ACE2 in stroke, randomly assigned rats (n = 16) are treated centrally for five days prior to and three days after stroke with the ACE2 inhibitor MLN-4760 (100 μM infused at a rate of 0.5 μL/h) or sterile saline (0.9%) via intracerebroventricular infusion. Following endothelin-1 MCAO, neurological function is assessed at 4 h, 1 d, and 3 d, and brains are harvested at 3 d post-stroke for infarct volume analysis as above[3]. |
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References: [1]. Dales NA, et al. Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors. J Am Chem Soc. 2002 Oct 9;124(40):11852-3. |
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| Cas No. | 305335-31-3 | SDF | |
| 别名 | GL-1001 | ||
| Canonical SMILES | O=C(O)[C@H](CC1=CN=CN1CC2=CC(Cl)=CC(Cl)=C2)N[C@H](C(O)=O)CC(C)C | ||
| 分子式 | C19H23Cl2N3O4 | 分子量 | 428.31 |
| 溶解度 | DMSO: 200 mg/mL (466.95 mM) | 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 | 2.3348 mL | 11.6738 mL | 23.3476 mL |
| 5 mM | 0.467 mL | 2.3348 mL | 4.6695 mL |
| 10 mM | 0.2335 mL | 1.1674 mL | 2.3348 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。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet