FG2216 (Synonyms: IOX3, YM-311) |
カタログ番号GC16638
One-Click Copy Product Info
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FG2216 (IOX3) は、HIF プロリルヒドロキシラーゼ-2 (PHD2) の強力な経口活性阻害剤であり、IC50 は 3.9 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 223387-75-5
Sample solution is provided at 25 µL, 10mM.
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FG-2216 is a potent HIF-prolyl hydroxylase inhibitor. IC50 = 3.9 μM for PDH2 enzyme.
HIFs (hypoxia inducible factors) are transcription factor that activated by low oxygen availability. It leads to cellular, tissue and organismal adaptive response to hypoxia. Increased hemoglobin
levels are associated with intrauterine hypoxia. In cooperation with other transcriptional coactivators, HIF induces transcription of genes that ameliorate the effects of hypoxia, including erythropoietin and its receptor.
In rhesus macaques, FG-2216 reversibly activates endogenous erythropoietin (82- to 309-fold at 60 mg/kg), and as early as 4 hours after oral administration of FG-2216, circulating plasma Epo levels increases. [1]
Chronic administration of FG-2216 is well tolerated and induces erythropoiesis in rhesus macaques. It also induced a small elevation of hemoglobin expression in vivo. FG-2216–treated animals exerts rise in the percentage of hemoglobin-containing reticulocytes (% F+ retics) 1 to 2 weeks after chronic dosing began. [1]
Reference:
1. Hsieh MM, Linde NS, Wynter A 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.
| Cas No. | 223387-75-5 | SDF | |
| 同義語 | IOX3, YM-311 | ||
| Chemical Name | (Z)-2-(((1-chloro-4-hydroxyisoquinolin-3-yl)(hydroxy)methylene)amino)acetic acid | ||
| Canonical SMILES | ClC1=NC(/C(O)=N/CC(O)=O)=C(O)C2=CC=CC=C21 | ||
| Formula | C12H9ClN2O4 | M.Wt | 280.66 |
| 溶解度 | ≥ 14.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.563 mL | 17.8152 mL | 35.6303 mL |
| 5 mM | 712.6 μL | 3.563 mL | 7.1261 mL |
| 10 mM | 356.3 μL | 1.7815 mL | 3.563 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)