CL 82198 hydrochloride
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:10 μg/mL 时89%抑制
CL 82198是一种选择性的MMP-13抑制剂。
基质金属蛋白酶(MMPs)参与正常组织重建过程(如伤口愈合、怀孕和血管新生)相关的细胞外基质降解。MMPs的表达和活性由于其降解性而受到高度控制,这种调控的明显缺失导致结缔组织的病理破坏以及随之而来的疾病状态。
体外:CL-82198被鉴定为一种弱MMP-13抑制剂,对MMP-1、MMP-9或相关酶TACE没有活性。带有药物样特性,CL-82198被视为优化酶的效力和选择性的理想候选物。核磁共振结合研究表明,CL-82198结合MMP-13的整个S1'口袋,这是其对MMP-1、MMP-9和TACE的选择性的基础[1]。
体内:为研究MMP-13在乙酰氨基酚胃保护期间的下调作用,CL-82198对IBP诱导的胃损伤进行了评价。结果表明,在 IBP存在下,CL-82198剂量依赖性地降低胃损伤。与IBP单独给药相比,CL-82198给药0.2和1.0 mg/kg分别导致胃损伤下降40.3%和72.1%[1]。
临床试验:N/A
参考文献:
[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,μMonoi N,μMikoshiba S,Hirayama Y,Serizawa T,Adachi K,Koide M,Ohdera M,μMurakoshi 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.
Physical Appearance | A crystalline solid |
Storage | Desiccate at RT |
M.Wt | 338.83 |
Cas No. | 307002-71-7 |
Formula | C17H33N2O3·HCl |
Solubility | Soluble in DMSO |
Chemical Name | N-(4-morpholin-4-ylbutyl)-1-benzofuran-2-carboxamide;hydrochloride |
SDF | Download SDF |
Canonical SMILES | C1COCCN1CCCCNC(=O)C2=CC3=CC=CC=C3O2.Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |