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- 详细信息
- 文献和实验
- 技术资料
- 库存：
35
- 英文名：
CL 82198 hydrochloride
- CAS号：
307002-71-7
- 供应商：
上海莼试
- 保存条件：
Desiccate at RT
- 规格：
10mg 50mg
| 货号 | CS-01Y64197 | 规格 | 10mg 50mg |
| CAS号 | 307002-71-7 | 分子量 | 338.83 |
| 含量 | >98.00% | 别名 | |
| 分子式 | C17H33N2O3.HCl | 化学名 | N-(4-morpholin-4-ylbutyl)-1-benzofuran-2-carboxamide;hydrochloride |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
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:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
IC50: 89% inhibition at 10μg/mLCL 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/AReferences:[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.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
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文献和实验Preparing a Selenomethionyl Protein
1M IPTG M9 media (minimal media) 1 Liter 5x M9 media: (sterile filtered) 30g Na2 HPO4 or 64g Na2 HPO4 -7H2 O 15g KH2 PO4 5g NH4 Cl 2.5g NaCl Dilute and autoclave before use. Amino acid
Preparing a Selenomethionyl Protein
4 5g NH4 Cl 2.5g NaCl Dilute and autoclave before use. Amino acid 50x stock Use all amino acids EXCEPT Gly, Ala, Pro, Asn, Cys, and Met at a concentration of 2mg/ml To help in dissolving the amino acids, autoclave
Determination of Protein Contacts by Chemical Cross‐Linking With EDC and Mass Spectrometry
‐NHS;Pierce) in 50 mM MES; prepare immediately before use. 0.5 M hydroxylamine hydrochloride 25 mM Tris⋅Cl, pH
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