FG 2216
- Product Name
- FG 2216
- CAS No.
- 223387-75-5
- Chemical Name
- FG 2216
- Synonyms
- BIQ;IOX-3;YM 311;FG2216;FG-2216;FG 2216;CS-1687;FG-2216(IOX3;FG-2216 ，S7979;FG-2216 - YM 311
- CBNumber
- CB62666905
- Molecular Formula
- C12H9ClN2O4
- Formula Weight
- 280.66
- MOL File
- 223387-75-5.mol
FG 2216 Property
- Boiling point:
- 670.6±55.0 °C(Predicted)
- Density
- 1.571±0.06 g/cm3(Predicted)
- storage temp.
- -20°C
- solubility
- insoluble in H2O; ≥14.05 mg/mL in DMSO; ≥5.12 mg/mL in EtOH with ultrasonic
- form
- powder
- pka
- 3.20±0.10(Predicted)
- color
- white to beige
- 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)
- InChIKey
- OUQVKRKGTAUJQA-UHFFFAOYSA-N
- SMILES
- OC1=C(C(NCC(O)=O)=O)N=C(Cl)C2=CC=CC=C21
Safety
- WGK Germany
- WGK 3
- Storage Class
- 11 - Combustible Solids
- Hazard Classifications
- Eye Irrit. 2
Skin Irrit. 2
STOT SE 3
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML1811
- Product name
- BIQ
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $175
- Updated
- 2026/03/19
- Product number
- SML1811
- Product name
- BIQ
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $657
- Updated
- 2025/07/31
- Product number
- 18382
- Product name
- FG-2216
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $44
- Updated
- 2024/03/01
- Product number
- 18382
- Product name
- FG-2216
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $140
- Updated
- 2024/03/01
- Product number
- 18382
- Product name
- FG-2216
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $257
- Updated
- 2024/03/01
FG 2216 Chemical Properties,Usage,Production
Description
FG-2216 is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2; IC50 = 3.9 micromolar). It has been shown to reversibly stimulate erythropoietin secretion at 100 μM in vitro and to increase hematocrit, red blood cell count, and hemoglobin levels at 50 mg/kg in mice.
Uses
FG 2216 is an erythropoietic agent which is orally active prolyl-hydroxylase inhibitor which increases erythropoietin production in end-stage kidney disease.
Biochem/physiol Actions
BIQ (FG-2216) is an orally available and potent inhibitor of prolyl-hydroxylase (PHD). BIQ induces significant and reversible plasma erythropoietin (EPO) levels in vitro and in hemodialysis patients.
Synthesis
223388-21-4
616-34-2
223387-75-5
GENERAL METHODS: 1-chloro-4-hydroxyisoquinoline-3-carboxylic acid (300 mg, 1.35 mmol), methyl 2-aminoacetate (1.2 eq.), PyBOP (1.2 eq.), and triethylamine (Et3N, 1.5 mmol) were dissolved in anhydrous N,N-dimethylformamide (DMF, 5 mL) followed by stirring of the reaction for 24 h at room temperature. Upon completion of the reaction, DMF was removed by distillation under reduced pressure and the resulting residue was suspended in dichloromethane (CH2Cl2, 20 mL) and washed with deionized water (2 × 10 mL). The organic phase was dried over anhydrous magnesium sulfate (MgSO4), filtered and purified by column chromatography (using a Biotage SNAP KP-SIL TM 25g column with an elution system of cyclohexane/ethyl acetate, with the specific ratio adjusted according to the elution of each methyl ester). The purified product was dissolved in a solvent mixture of tetrahydrofuran (THF) and water (1:1, 10 mL), lithium hydroxide monohydrate (LiOH-H2O, 5 eq.) was added, and the reaction was stirred for 12 h at room temperature. Subsequently, THF was removed by distillation under reduced pressure and the remaining aqueous solution was neutralized with concentrated hydrochloric acid (HCl) to pH ≈ 7. If a precipitate was produced, the precipitate was collected by filtration and dried under vacuum to afford the target product 2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid (20). If no precipitate was formed, the aqueous solution was extracted with ethyl acetate (EtOAc, 3 x 10 mL), the organic layers were combined, dried over anhydrous magnesium sulfate (MgSO4), filtered and concentrated under reduced pressure to give the target product. Preparation of 2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)acetic acid (20): 1-chloro-4-hydroxyisoquinoline-3-carboxylic acid (300 mg, 1.35 mmol) was used as a starting material, and operated according to the above general method, the target compound (20) was finally obtained as a white solid (175 mg, 46% yield). Characterization data: 1H NMR (400 MHz, DMSO-d6) δ = 9.16 (t, J = 6.0 Hz, 1H, NH), 8.30 (m, 1H, ArH), 8.24 (m, 1H, ArH), 7.84-8.09 (m, 2H, ArH), 4.02 (d, J = 6.0 Hz, 2H, CH2) ppm. 13C NMR (101 MHz, DMSO-d6) δ = 171.4, 169.6, 155.1, 139.4, 132.6, 132.5, 130.3, 129.3, 126.9, 123.8, 121.3, 41.7 ppm. Melting Point (Mp): 212-214°C. High Resolution Mass Spectrometry (HRMS, ESI-TOF) Calculated value C12H9ClN2NaO4 [M + Na+]: 303.0144, measured value: 303.0143. Fourier transform infrared spectra (FT-IR, neat) νmax: 3402, 2915, 1712, 1641, 1354, 1255, 794 cm1.
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].
| 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. |
References
1. hsieh mm, linde ns, wynter a et al. hif prolyl hydroxylase inhibitionresults in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. blood. 2007 sep 15;110(6):2140-7.
FG 2216 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from FG 2216 manufacturers
- Product
- FG 2216 223387-75-5
- Price
- US $1.00/g
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 20kg
- Release date
- 2019-12-23