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

FG-2216  (Synonyms: IOX3; YM311)

Cat. No.: HY-15641 Purity: 99.49%
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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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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 110 In-stock
25 mg USD 220 In-stock
50 mg USD 319 In-stock
100 mg USD 539 In-stock
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Based on 3 publication(s) in Google Scholar

FG-2216 Related Antibodies

Top Publications Citing Use of Products

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

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HIF-1α HIF

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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]
Cellular Effect
Cell Line Type Value Description References
Hep 3B2 IC50
3.9 μM
Compound: FG-2216
Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA
Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA
[PMID: 24894560]
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].

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

FG-2216 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CNC(C1=C(O)C2=C(C(Cl)=N1)C=CC=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (178.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (8.91 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5630 mL 17.8151 mL 35.6303 mL 89.0757 mL
5 mM 0.7126 mL 3.5630 mL 7.1261 mL 17.8151 mL
10 mM 0.3563 mL 1.7815 mL 3.5630 mL 8.9076 mL
15 mM 0.2375 mL 1.1877 mL 2.3754 mL 5.9384 mL
20 mM 0.1782 mL 0.8908 mL 1.7815 mL 4.4538 mL
25 mM 0.1425 mL 0.7126 mL 1.4252 mL 3.5630 mL
30 mM 0.1188 mL 0.5938 mL 1.1877 mL 2.9692 mL
40 mM 0.0891 mL 0.4454 mL 0.8908 mL 2.2269 mL
50 mM 0.0713 mL 0.3563 mL 0.7126 mL 1.7815 mL
60 mM 0.0594 mL 0.2969 mL 0.5938 mL 1.4846 mL
80 mM 0.0445 mL 0.2227 mL 0.4454 mL 1.1134 mL
100 mM 0.0356 mL 0.1782 mL 0.3563 mL 0.8908 mL
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FG-2216 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FG-2216223387-75-5IOX3 YM311FG2216FG 2216IOX 3IOX-3YM311YM 311YM-311HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHHIFprolylhydroxylasePHD2erythropoietinfetalhemoglobinInhibitorinhibitorinhibit

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