| 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 |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京