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• 产品描述： FG-2216 (IOX3) is a potent and orally active inhibitor of HIF prolyl hydroxylase-2 (PHD2), with an IC50 of 3.9 μM. FG-2216 induces robust erythropoietin and modest fetal hemoglobin in vivo

• 靶点： IC50: 3.9 nM (PHD2);HIF/HIFProlyl-Hydroxylase

• 体外研究：
  FG-2216 (50-100 μM; 24 h) stimulates erythropoietin (Epo) secretion by PHD2 inhibition in Hep3B cells. FG-2216 (3-100 μM; 24 h) stabilizes HIF-1α and HIF-2α in Hep3B cells

• 体内研究：
  FG-2216 (40-60 mg/kg; p.o. twice a week for 150 d) induces erythropoiesis and a small elevation of hemoglobin (HbF) expression, and is well tolerated in rhesus macaques. FG-2216 (50 mg/kg; p.o. once daily for 4 or 12 d) increases hematocrit, red blood cell counts, and hemoglobin levels in mice. FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques. Animal Model: Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation Dosage: 40, 60 mg/kg Administration: P.o. (40 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeksP.o. (60 mg/kg) twice a week for 6-8 weeks Result: Exhibited reticulocytosis within 1-2 weeks of dosing.Increased total hemoglobin levels at the end of the study duration.

• 参考文献：
  1. Hong YR, et al. [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7. 2. Hsieh MM, et al. HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. Blood. 2007 Sep 15;110(6):2140-7. 3. Bernhardt WM, et, al. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD. J Am Soc Nephrol. 2010 Dec;21(12):2151-6.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.563 ml	17.815 ml	35.63 ml
  5 mM	0.713 ml	3.563 ml	7.126 ml
  10 mM	0.356 ml	1.781 ml	3.563 ml
  50 mM	0.071 ml	0.356 ml	0.713 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 *