貨號	規(guī)格	價格	上海	北京	武漢	南京
S81438-2mg	97.2%	￥230.00 S81438-2mg ￥230.00 現(xiàn)貨	5 5	-	-	-
S81438-5mg	97.2%	￥360.00 S81438-5mg ￥360.00 現(xiàn)貨	6 6	-	-	-
S81438-10mg	97.2%	￥610.00 S81438-10mg ￥610.00 現(xiàn)貨	5 5	-	-	-
S81438-25mg	97.2%	￥1150.00 S81438-25mg ￥1150.00 現(xiàn)貨	6 6	-	-	-
S81438-50mg	≥97%	￥1660.00 S81438-50mg ￥1660.00 2-3天	0 貨期：2-3天	-	-	-
S81438-100mg	≥97%	￥2950.00 S81438-100mg ￥2950.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

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

產(chǎn)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

靶點：

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

體外研究：

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

體內(nèi)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.

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻

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