FG-2216

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

FG-2216 (YM-311, IOX3) 是一种 HIF 脯氨酰羟化酶的选择性小分子抑制剂，IC50 为 3.9 nM (PDH2)。

FG-2216 (YM-311, IOX3) is a selective small molecule inhibitor of HIF prolyl hydroxylase with IC50 of 3.9 nM (PDH2), decreases protein expression of DNA/RNA demethylase FTO (in C2C12 cells) and reduces maximal respiration rate in vitro; up-regulates HIF-1α and increases erythropoietin expression in mice, also significantly reduces bone mineral density and content and alter adipose tissue distribution in mice; FG-2216 is orally bioavailable and induced significant and reversible Epo induction in vivo.(In Vitro):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.(In Vivo):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.

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.

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 weeks P.o. (60 mg/kg) twice a week for 6-8 weeks P.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.

YM-311 | IOX3

Angiogenesis

HIF/HIF Prolyl-hydroxylase

PHD2

Other Indications

——

223387-75-5

280.7

C12H9ClN2O4

>98% (HPLC)

DMSO: ≥ 31 mg/mL

OC1=C(C(NCC(O)=O)=O)N=C(Cl)C2=CC=CC=C21

Glycine, N-[(1-chloro-4-hydroxy-3-isoquinolinyl)carbonyl]-

(-20℃)

With Ice Pack

≥ 2 years