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- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
UK-383367
- 库存：
999
- 供应商：
北京索莱宝科技有限公司
- CAS号：
348622-88-8
- 规格：
5mg/10mg
| 规格： | 5mg | 产品价格： | ¥1190.00 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ¥1990.00 |
| CAS | 348622-88-8 |
| 英文名称 | UK-383367 |
| 分子式 | C15H24N4O4 |
| 分子量 | 324.38 |
| 规格 | 5mg ; 10mg |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 级别 | Cell Culture |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷冻运输 |
| EC | 683-685-4 |
| MDL | MFCD19690945 |
| SMILES | NC(C1=NOC([C@H](CCCC2CCCCC2)CC(NO)=O)=N1)=O |
| InChIKey | ARJCBSRIPGJMAD-LLVKDONJSA-N |
| InChI | InChI=1S/C15H24N4O4/c16-13(21)14-17-15(23-19-14)11(9-12(20)18-22)8-4-7-10-5-2-1-3-6-10/h10-11，22H，1-9H2，(H2，16，21)(H，18，20)/t11-/m1/s1 |
| PubChem CID | 9818682 |
| 靶点 | Procollagen C Proteinase |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | 是procollagen C-proteinase抑制剂,对MMPs具有优异的选择性。 |
| 生物活性 | UK-383367 is an orally available pro-collagen C-protease inhibitor (BMP-1) with an IC50 value of 44 nM. UK-383367 can reduce renal fibrosis and inflammation in chronic kidney disease (CKD) and may be used to study postoperative skin scarring[1][2][3]. |
| In Vitro | UK383，367 pretreatment inhibited the induction of collagen type I/III， fibronectin， and α-smooth muscle actin in both mouse proximal tubular cells and NRK-49F cells treated with transforming growth factor-β1.[1]。Cell Viability Assay[1]:Cell Line: mPTCs induced by TGF-β;Concentration: 0， 100， 200， 300， 400， 800， 1000 nM;Incubation Time: 24 h;Result:Inhibited cell proliferation.Western Blot Analysis[1]:Cell Line:mPTCs induced by TGF-β， NRK-49F;Concentration:100， 200 nM;Incubation Time:30 min;Result:Inhibited the induction of collagen I/III， fibronectin， and α-SMA in cells， blocked the activation of NRK-49F cells， and blocked the activation of NRK-49F renal fibroblasts. |
| In Vivo | UK - 383，367 (5 - {(1R)-4 - cyclohexyl - 1 - [2 - (hydroxyamino)-2 - oxoethyl]butyl}-1，2，4 - oxadiazole - 3 - carboxamide) is a novel procollagen C - proteinase inhibitor evaluated for the treatment of post - surgical dermal scarring. It is extensively metabolized in rat and dog absorption， distribution， metabolism and excretion studies， and a metabolic pathway for UK - 383，367 was determined. A long - lived metabolite was identified in dog plasma.[2]Animal Model: Unilateral Ureteral Obstruction (UUO) CKD mouse model[1];Dosage: 5 mg/kg， daily， 7 days;Administration:Intraperitoneal injection (i.p.);Result:Improved the fibrosis in small ducts， reduced the deposition of collagen I， collagen III， and fibronectin (FN)， and it suppressed the upregulation of α-SMA， lessening the expression of the inflammatory markers IL-1β and MCP1. |
| 数据来源文献 | [1]. Mi Bai， et al. BMP1 inhibitor UK383，367 attenuates renal fibrosis and inflammation in CKD. Am J Physiol Renal Physiol. 2019 Dec 1;317(6):F1430-F1438. [2]. Allan GA， et al. Pharmacokinetics and metabolism of UK-383，367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica. 2006 May;36(5):399-418. [3]. Eugenia C Salcedo， et al. Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer. ACS Chem Biol. 2021 Apr 16;16(4):712-723. |
| 单位 | 瓶 |
| 表格1 | |*|1mg|5mg|10mg|$$|1mM|3.0828mL|15.414mL|30.828mL|$$|5mM|0.6166mL|3.0828mL|6.1656mL|$$|10mM|0.3083mL|1.5414mL|3.0828mL| |
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