FG-2216
Based on 6 publication(s) in Google Scholar
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.
- Purity: 99.46%
- CAS No.: 223387-75-5
- Formula: C12H9ClN2O4
- Molecular Weight:280.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) FG-2216
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Biological Activity
IC50: 3.9 nM (PHD2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | EC50 |
64 μM
Compound: FG-2216
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Hepatoprotective activity against human Hep3B cells assessed as increase of erythropoietin release by measuring effective concentration
Hepatoprotective activity against human Hep3B cells assessed as increase of erythropoietin release by measuring effective concentration
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[PMID: 38754564] |
| Hep 3B2 | IC50 |
3.9 μM
Compound: FG-2216
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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
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[PMID: 24894560] |
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.
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Animal Model:Male rhesus macaques (3-6 years; 4-7 kg) mice are treated with large-volume phlebotomy with iron supplementation[2]
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Dosage:40, 60 mg/kg
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 223387-75-5
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Appearance Solid
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Molecular Weight 280.66
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Formula C12H9ClN2O4
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Color White to off-white
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SMILES
O=C(O)CNC(C1=C(O)C2=C(C(Cl)=N1)C=CC=C2)=O
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Synonyms
IOX3; YM311
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
ACS Omega
UHPLC-HRMS Method for the Simultaneous Screening of 235 Drugs in Capillary Blood for Doping Control Purpose: Comparative Evaluation of Volumetric and Non-volumetric Dried Blood Spotting Devices. [Abstract]2022 Aug 29;7(36):31845-31868. PMID: 36119994 -
Metallomics
2024 Oct 4;16(10):mfae044. PMID: 39317669 -
J Anal Toxicol
2021 Feb 13;45(2):184-194. PMID: 32435795 -
Biomed Chromatogr
Automated sample preparation for the detection and confirmation of hypoxia-inducible factor stabilizers in urine. [Abstract]2021 Feb;35(2):e4970. PMID: 32840903 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hong YR, 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. [Content Brief]
[2]. Hsieh MM, 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. [Content Brief]
[3]. Bernhardt WM, et, al. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD. J Am Soc Nephrol. 2010 Dec;21(12):2151-6. [Content Brief]
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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