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• 产品描述： VH298 是一种有效的 VHL (Von Hippel-Lindau, the E3 ligase) 的抑制剂，可稳定 HIF-α。VH298 可阻断VHL:HIF-α的相互作用，在等温滴定热分析 (ITC) 中的Kd值为90 nM、在竞争性荧光偏振测定中的Kd值为80 nM。VH-298可用于PROTAC技术

• 靶点： VHL:HIF-α(competitive fluorescence polarization assay):80 nM(Kd); VHL:HIF-α(isothermal titration calorimetry (ITC)):90 nM(Kd);Others; HIF; LigandforE3Ligase

• 体外研究：
  VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC

• 体内研究：
  VH298 can activate the HIF-1 signalling pathway by stabilizing both forms of HIF-1α in vitro. VH298 promotes rFb variability, migration, and synthesis of collagen and regulatory cell factors. VH298 improves the angiogenesis of hUVEC

• 细胞实验： Cell lines: rFb cells, hUVEC cells Concentrations: 10 μM, 30 μM, 100 μM, 200 μM Incubation Time: 48 h Method: The rFb are trypsinised and placed in flat-bottomed 96-well plates at an initial density of 5000 cells per well. After 24 h of incubation, the medium is changed to VH298-containing medium at different dosages (0 μM, 10 μM, 30 μM, 100 μM, and 200 μM). rFb are incubated at 37°C for 48 h. The proliferation is determined by the Cell Counting Kit-8 (CCK-8) assay. After incubation, rFb are treated with the CCK-8 solution at a final concentration of 10% for 2 h at 37°C, followed by measurement of absorbance at 450nm using a microplate reader.

• 动物实验： Animal Models: Sprague-Dawley rats intraperitoneal injected of streptozotocin at 65 mg/kg Dosages: 30 μM VH298 in PBS (100 microlitres) Administration: local injection

• 参考文献：
  1. Julianty Frost, et al. Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition. Nat Commun. 2016 Nov 4;7:13312. 2. Shuo Qiu, et al. Von Hippel-Lindau (VHL) Protein Antagonist VH298 Improves Wound Healing in Streptozotocin-Induced Hyperglycaemic Rats by Activating Hypoxia-Inducible Factor- (HIF-) 1 Signalling. J Diabetes Res. 2019 Feb 17;2019:1897174.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.91 ml	9.548 ml	19.097 ml
  5 mM	0.382 ml	1.91 ml	3.819 ml
  10 mM	0.191 ml	0.955 ml	1.91 ml
  50 mM	0.038 ml	0.191 ml	0.382 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *