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• 产品描述： PFI-2 ((R)-PFI-2 hydrochloride) hydrochloride is a potent and selective SET domain containing lysine methyltransferase 7 (SETD7) inhibitor. (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM. PFI-2 hydrochloride can be used for the research of chronic kidney disease and inflammation response in the development of renal fibrosis

• 靶点： Histone Methyltransferase;HistoneMethyltransferase

• 体外研究：
  (R)-PFI-2 shows high inhibiting activity with IC50 value of 2.0  nM and (S)-PFI-2 shows inhibiting activity with IC50  value of 1.0  μM

• 体内研究：
  PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuates the progression of renal fibrosis and preserves renal function in FA nephropathy. PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced ECM accumulation and fibroblasts activation after FA injury[2]. PFI-2 hydrochloride (i.p., 200 μM, twice a week) impeded Th2 cytokine signaling activation and M2 macrophage polarization. PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed M2 macrophages-myofibroblasts transition and myeloid myofibroblasts accumulation in the FA-treated kidneys. PFI-2 hydrochloride (i.p., 200 μM, twice a week) attenuated macrophages M2 polarization and M2 macrophages-to-myofibroblasts transition in obstructed kidneys. PFI-2 hydrochloride (i.p., 200 μM, twice a week) suppressed myeloid myofibroblast accumulation and renal fibrosis after UUO injury. PFI-2 hydrochloride (i.p., 200 μM, twice a week) reduced the infiltration of inflammatory cells, the production of inflammatory molecules, and NF-κB activation in FA nephropathy. Animal Model: Male C57BL/6 mice (8-10-week old, 20-25 g) Dosage: 200 μM (PFI-2 is diluted in 100 μL 0.1% (v/v) DMSO to a concentration of 200 μM/100 μL) Administration: intraperitoneal injection, twice a week Result: Presented less bone marrow-derived myofibroblasts, fewer CD206+/α-smooth muscle actin + cells and developed less renal fibrosis (P<0.01).Reduced the infiltration of inflammatory cells and decreased the production of pro-inflammatory cytokines and chemokines in the kidneys

• 参考文献：
  1. Yuzhen Niu, et al. Revealing inhibition difference between PFI-2 enantiomers against SETD7 by molecular dynamics simulations, binding free energy calculations and unbinding pathway analysis. Sci Rep. 2017 Apr 18;7:46547. 2. Benquan Liu, et al. Pharmacological inhibition of SETD7 by PFI-2 attenuates renal fibrosis following folic acid and obstruction injury. Eur J Pharmacol. 2021 Jun 15;901:174097.

• 溶解性： Soluble  in  DMSO、H2O

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.866 ml	9.329 ml	18.657 ml
  5 mM	0.373 ml	1.866 ml	3.731 ml
  10 mM	0.187 ml	0.933 ml	1.866 ml
  50 mM	0.037 ml	0.187 ml	0.373 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 *