FG2216HIF-prolyl hydroxylase inhibitor CAS# 223387-75-5 |
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Quality Control & MSDS
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| Cas No. | 223387-75-5 | SDF | Download SDF |
| PubChem ID | 6914666 | Appearance | Powder |
| Formula | C12H9ClN2O4 | M.Wt | 280.66 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | YM-311 | ||
| Solubility | DMSO : ≥ 31 mg/mL (110.45 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[(1-chloro-4-hydroxyisoquinoline-3-carbonyl)amino]acetic acid | ||
| SMILES | C1=CC=C2C(=C1)C(=C(N=C2Cl)C(=O)NCC(=O)O)O | ||
| Standard InChIKey | OUQVKRKGTAUJQA-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.
IC50 value: 3.9 uM [1]
Target: PDH inhibitor
FG-2216 was orally bioavailable and induced significant and reversible Epo induction in vivo (82- to 309-fold at 60 mg/kg). Chronic oral dosing in male rhesus macaques was well tolerated, significantly increased erythropoiesis, and prevented anemia induced by weekly phlebotomy. Furthermore, modest increases in HbF-containing red cells and reticulocytes were demonstrated by flow cytometry, though significant increases in HbF were not demonstrated by high-pressure liquid chromatography (HPLC) [2]. References: | |||||
FG2216 Dilution Calculator
FG2216 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.563 mL | 17.8152 mL | 35.6303 mL | 71.2606 mL | 89.0758 mL |
| 5 mM | 0.7126 mL | 3.563 mL | 7.1261 mL | 14.2521 mL | 17.8152 mL |
| 10 mM | 0.3563 mL | 1.7815 mL | 3.563 mL | 7.1261 mL | 8.9076 mL |
| 50 mM | 0.0713 mL | 0.3563 mL | 0.7126 mL | 1.4252 mL | 1.7815 mL |
| 100 mM | 0.0356 mL | 0.1782 mL | 0.3563 mL | 0.7126 mL | 0.8908 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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