1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. FG-2216

FG-2216 (Synonyms: IOX3; YM311)

Cat. No.: HY-15641 Purity: 99.32%
Handling Instructions

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.

For research use only. We do not sell to patients.

FG-2216 Chemical Structure

FG-2216 Chemical Structure

CAS No. : 223387-75-5

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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
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Estimated Time of Arrival: December 31
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5 mg USD 66 In-stock
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10 mg USD 110 In-stock
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25 mg USD 220 In-stock
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50 mg USD 319 In-stock
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100 mg USD 539 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

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[1][2][3].

IC50 & Target

IC50: 3.9 nM (PHD2)[1]

In Vitro

FG-2216 (50-100 μM; 24 h) stimulates erythropoietin (Epo) secretion by PHD2 inhibition in Hep3B cells[1].
FG-2216 (3-100 μM; 24 h) stabilizes HIF-1α and HIF-2α in Hep3B cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[2].
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[1].
FG-2216 (40-60 mg/kg; a single p.o) reversibly induces endogenous Epo in rhesus macaques[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation[2]
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.
Clinical Trial
Molecular Weight

280.66

Formula

C12H9ClN2O4

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (110.45 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5630 mL 17.8151 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
FG-2216
Cat. No.:
HY-15641
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