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FG2216

现货
Catalog No.
B5851
HIF-脯氨酰羟化酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,100.00
现货
5mg
¥ 1,200.00
现货
25mg
¥ 4,100.00
现货

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Background

FG-2216 is a potent HIF-prolyl hydroxylase inhibitor. IC50 = 3.9 μM for PDH2 enzyme.

HIFs (hypoxia inducible factors) are transcription factor that activated by low oxygen availability. It leads to cellular, tissue and organismal adaptive response to hypoxia. Increased hemoglobin

levels are associated with intrauterine hypoxia. In cooperation with other transcriptional coactivators, HIF induces transcription of genes that ameliorate the effects of hypoxia, including erythropoietin and its receptor.

In rhesus macaques, FG-2216 reversibly activates endogenous erythropoietin (82- to 309-fold at 60 mg/kg), and as early as 4 hours after oral administration of FG-2216, circulating plasma Epo levels increases. [1]

Chronic administration of FG-2216 is well tolerated and induces erythropoiesis in rhesus macaques. It also induced a small elevation of hemoglobin expression in vivo. FG-2216–treated animals exerts rise in the percentage of hemoglobin-containing reticulocytes (% F+ retics) 1 to 2 weeks after chronic dosing began. [1]

Reference:
1.  Hsieh MM, Linde NS, Wynter A 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt280.66
Cas No.223387-75-5
FormulaC12H9ClN2O4
Solubility≥14.05mg/mL in DMSO
Chemical Name(Z)-2-(((1-chloro-4-hydroxyisoquinolin-3-yl)(hydroxy)methylene)amino)acetic acid
SDFDownload SDF
Canonical SMILESClC1=NC(/C(O)=N/CC(O)=O)=C(O)C2=CC=CC=C21
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

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