CL 82198 hydrochloride
目录号 : GC15952
An inhibitor of MMP-13
Cas No.:1188890-36-9
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
IC50: 89% inhibition at 10μg/mL
CL 82198 is a selective MMP-13 inhibitor.
Matrix metalloproteinases (MMPs) are involved in the degradation of the extracellular matrix associated with normal tissue remodeling processes such as wound healing, pregnancy, and angiogenesis. Expression and activity of MMPs is highly controlled due to their degradative nature where the apparent loss in this regulation leads to the pathological destruction of connective tissue and the ensuing disease state.
In vitro: CL-82198 was identified as a weak inhibitor against MMP-13 and demonstrated no activity against MMP-1, MMP-9, or the related enzyme TACE. Bearing drug-like properties, CL-82198 was regarded as an ideal candidate for optimization of enzyme potency and selectivity. In NMR binding studies, it was shown that CL-82198 bound within the entire S1’ pocket of MMP-13, which was the basis of its selectivity against MMP-1, MMP-9, and TACE [1].
In vivo: To investigate the contribution of MMP-13 down-regulation during gastroprotection by acetaminophen, the effects of CL-82198 on IBP-induced gastric damage were evaluated. Results showed that CL-82198 decreased gastric lesions in a dose-dependent manner in the presence of IBP. Compared with IBP administration alone, CL-82198 administered at 0.2 and 1.0 mg/kg resulted in 40.3% and 72.1% decrease in gastric lesion, respectively [1].
Clinical trial: N/A
References:
[1] James M. Chen,Frances C. Nelson,Jeremy I. Levin,Dominick Mobilio,Franklin J. Moy,Ramaswamy Nilakantan,Arie Zask,andRobert Powers. Structure-Based Design of a Novel, Potent, and Selective Inhibitor for MMP-13 Utilizing NMR Spectroscopy and Computer-Aided Molecular Design. J. Am. Chem. Soc.,2000,122(40), pp 9648–9654
[2] Fukushima E,Monoi N,Mikoshiba S,Hirayama Y,Serizawa T,Adachi K,Koide M,Ohdera M,Murakoshi M,Kato H. Protective effects of acetaminophen on ibuprofen-induced gastric mucosal damage in rats with associated suppression of matrix metalloproteinase. J Pharmacol Exp Ther.2014 Apr;349(1):165-73.
| Cas No. | 1188890-36-9 | SDF | |
| 化学名 | N-(4-morpholin-4-ylbutyl)-1-benzofuran-2-carboxamide;hydrochloride | ||
| Canonical SMILES | C1COCCN1CCCCNC(=O)C2=CC3=CC=CC=C3O2.Cl | ||
| 分子式 | C17H33N2O3.HCl | 分子量 | 338.83 |
| 溶解度 | DMF: 3 mg/ml,DMSO: 2.5 mg/ml,Ethanol: 25 mg/ml,PBS (pH 7.2): 0.25 mg/ml | 储存条件 | Desiccate at RT |
| 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 | 2.9513 mL | 14.7567 mL | 29.5133 mL |
| 5 mM | 0.5903 mL | 2.9513 mL | 5.9027 mL |
| 10 mM | 0.2951 mL | 1.4757 mL | 2.9513 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。