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UK 383367
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
UK 383367图片
CAS NO:348622-88-8
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
UK 383367 (UK 383367) 是一种有效的选择性 BMP-1(前胶原 C 蛋白酶)抑制剂,IC50 为 44 nM;对 BMP-1 的选择性优于 MMP 1、2、3、9 和 14(列出的 MMP 的 IC50 值 \u003e10,000 nM)。
Cas No.348622-88-8
别名UK383367, UK-383367
化学名5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide
Canonical SMILESC1CCC(CC1)CCCC(CC(=O)NO)C2=NC(=NO2)C(=O)N
分子式C15H24N4O4
分子量324.38
溶解度DMF: 16 mg/mL,DMSO: 25 mg/mL,DMSO:PBS (pH 7.2)(1:5): 0.16 mg/mL,Ethanol: 16 mg/mL
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

UK 383367 is a novel procollagen C-protein (PCP) inhibitor being investigated for the treatment of post-surgical dermal scarring, which potently inhibits the activity of PCP with the value of 50% inhibition concentration IC50of 44 nM, as well as a selective inhibitor of matrix metalloproteinases (MMPs) with values of IC50>60,000 nM for MMP-2 and >10,000 nM for MMP-1, MMP-3, MMP-9 and MMP-4. Although the mechanism is not clear yet, UK 383367 also exhibits weak inhibitory effects against phosphodiesterase-4 (PDE-4) enzyme, including PDE-4a, PDE-4b, PDE-4c and PDE-4d, with values of IC50of 1.8 μM, 1.5 μM, 2.4 μM and 0.9 μM respectively.

Reference

[1].G. A. Allan, J. I. Gedge, A. N. R. Nedderman, S. J. Roffey, H. F. Small and R. Webster. Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica 2006; 36(5): 399-418
[2].Bailey S, Fish PV, Billotte S, Bordner J, Greiling D, James K, McElroy A, Mills JE, Reed C, Webster R.ff. Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. Bioorg Med Chem Lett. 2008;18(24):6562-6567