|2-(1-氯-4-羟基异喹啉-3-甲酰胺)乙酸|CsnPharm

CAS No.: 223387-75-5

FG-2216 Catalog No. CSN16866

Synonyms: IOX3;YM311

FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 μM for PHD2 enzyme, orally bioavailable and induced significant and reversible Epo induction in vivo.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HIF PHD2

IC50:3.9μM
描述The family of HIF-PH (HIF prolyl hydroxylase) enzymes are the main molecular to regulate HIF activity through hydroxylation at 2 proline residues and cause the degradation of HIF, thus leading to inhibition on accumulation of functional HIF under normoxia. FG-2216 is the PHD inhibitor with IC50 value of 3.9μM for PHD2 (measure by SAR study). Treatment with FG-2216 for 24h can stabilize HIF-1α and HIF-2α in Hep3B cells. Significant increase of EPO, as well as obvious band of HIF-1α and HIF-2α can be observed in Hep3B cells treated with 100μM FG-2216 for 24h^[1]. Pre-treatment with FG-2216 at dose of 25 or 50mg/kg, b.w., i.p., 6h prior to initiation of ischaemia, caused HIF-1α and HIF-2α accumulation in kidney of rats, accompanied with increased transcriptional level of HIF targeted gene EPO and Glut-1^[2]. FG-2216 increased hemoglobin in healthy volunteers and hemodialysis patients with CKD in a phase IIa study. Thus, it was regarded as the lead drug candidate for the treatment of CKD-related anaemia^[3].
作用机制FG-2216 can bind with the catalytically active domain of human PHD2 and fill the empty spaces with hydrophobic functional groups.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	-	Inhibition of WNT3A signaling in HEK293 cells by luciferase reporter gene assay in presence of forskolin, IC50=3.5 nM	23844574
Hep3B cells	-	Function assay	-	Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA, IC50=3.9 μM	24894560
Hep3B cells	100 uM	Function assay	24 h	Inhibition of PHD2 in human Hep3B cells assessed as increase in erythropoietin secretion at 100 uM after 24 hrs by ELISA	24894560

动物研究
剂量
Mice^[4] (p.o.): 40 mg/kg, 60 mg/kg

给药途径
p.o.
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00456053 Renal Anemia Phase 2 Completed - -
参考文献

动物研究
剂量	Mice^[4] (p.o.): 40 mg/kg, 60 mg/kg
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00456053	Renal Anemia	Phase 2	Completed	-	-

[1] Hong YR, Kim HT, 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] Wang Z, Schley G, et al. The protective effect of prolyl-hydroxylase inhibition against renal ischaemia requires application prior to ischaemia but is superior to EPO treatment. Nephrol Dial Transplant. 2012 Mar;27(3):929-36.
[3] Locatelli F, Fishbane S, et al. Targeting Hypoxia-Inducible Factors for the Treatment of Anemia in Chronic Kidney Disease Patients. Am J Nephrol. 2017;45(3):187-199.
[4] Hsieh MM, Linde NS, et al. HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. Blood. 2007;110(6):2140-7.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5630 mL
- 17.8152 mL
- 35.6303 mL
- 5 mM
- 0.7126 mL
- 3.5630 mL
- 7.1261 mL
- 10 mM
- 0.3563 mL
- 1.7815 mL
- 3.5630 mL

技术信息

CAS号

223387-75-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H9ClN2O4

运输

蓝冰

分子量

280.66

别名

IOX3;YM311

溶解度

DMSO	46.0 mg/mL (163.9 mM)
Water	insoluble

动物实验配方

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