UK 383367
(Synonyms: UK383367, UK-383367) 目录号 : GC11366
A potent, selective BMP1 inhibitor
Cas No.:348622-88-8
Sample solution is provided at 25 µL, 10mM.
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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 IC50 of 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 IC50 of 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
| Cas No. | 348622-88-8 | SDF | |
| 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 SMILES | C1CCC(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°C |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.0828 mL | 15.414 mL | 30.828 mL |
| 5 mM | 0.6166 mL | 3.0828 mL | 6.1656 mL |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0828 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet