ML132 (NCGC 00185682)
(Synonyms: NCGC-00183434) 目录号 : GC33309
ML132 (NCGC 00185682) (NCGC-00183434) 是一种选择性 caspase 1 抑制剂，IC50 为 34.9 nM。
Cas No.:1230628-71-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM.
[1]. Boxer MB, et al. A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety. ChemMedChem. 2010 May 3;5(5):730-8.
| Cas No. | 1230628-71-3 | SDF | |
| 别名 | NCGC-00183434 | ||
| Canonical SMILES | ClC1=CC(C(N[C@@H](C(C)(C)C)C(N2CCC[C@H]2C(N[C@@H](CC(O)=O)C#N)=O)=O)=O)=CC=C1N | ||
| 分子式 | C22H28ClN5O5 | 分子量 | 477.94 |
| 溶解度 | Soluble in DMSO | 储存条件 | -80°C, protect from light, stored under nitrogen |
| 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 | 2.0923 mL | 10.4616 mL | 20.9231 mL |
| 5 mM | 0.4185 mL | 2.0923 mL | 4.1846 mL |
| 10 mM | 0.2092 mL | 1.0462 mL | 2.0923 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。
A small molecule inhibitor of Caspase 1
PMID:21735610DOI:NBK56241
A nitrile-containing propionic acid moiety as an electrophile for covalent attack by the active site cysteine residue of caspase 1 was investigated. Several cyanopropanate containing small molecules were synthesized, including one based upon the optimized peptidic scaffold of the prodrug VX-765. A number of these compounds were potent inhibitors of caspase 1 (IC50s ≤ 1 nM). Examination of these small molecules versus a caspase panel demonstrated an impressive degree of selectivity for caspase 1 inhibition. The small molecular probe ML132 (CID-4462093; NCGC-00183434) is the most potent caspase 1 inhibitor reported to date. It also possesses a unique selectivity pattern relative to other reported caspase inhibitors. A number of these compounds were assessed for their hydrolytic stability and selected absorption, distribution, metabolism and elimination (ADME) properties.