CAS NO: | 223387-75-5 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 280.66 |
Formula | C12H9ClN2O4 |
CAS No. | 223387-75-5 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 56 mg/mL (199.5 mM) |
Water:<1 mg/mL | |
Ethanol:<1 mg/mL | |
Solubility (In vivo) | Chemical Name: (1-chloro-4-hydroxyisoquinoline-3-carbonyl)glycine InChi Key: OUQVKRKGTAUJQA-UHFFFAOYSA-N InChi Code: 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) SMILES Code: OC1=C(C(NCC(O)=O)=O)N=C(Cl)C2=CC=CC=C21 |
Synonyms | IOX3; IOX 3; IOX-3; FG-2216; FG 2216; FG2216; YM311; YM-311; YM 311. |
In Vitro | In vitro activity: FG-2216 (IOX3; YM311) 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. Cell Assay: FG-2216 showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count |
In Vivo | In male rhesus macaques, FG-2216 (60 mg/kg, p.o.), induces significant and reversible Epo induction, and induces a small elevation of HbF expression. |
Animal model | Male rhesus macaques |
Formulation & Dosage | Suspended in 0.5% carboxymethylcellulose (CMC); 60 mg/kg; p.o. |
References | Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7; Blood. 2007 Sep 15;110(6):2140-7. |
Epo-induction in rhesus macques. (A) Circulating plasma Epo levels after a single oral dose of FG-2216. Blood. 2007 Sep 15;110(6):2140-7. |
| Hemoglobin increases by PHI. (A) Hemoglobin (g/dL) values are presented with respect to number of days on treatment in 1 rhesus macaque treated with FG-2216 (●) and 1 control animal (○). (B) Hemoglobin levels in treated and control rhesus macaques. Blood.2007 Sep 15;110(6):2140-7. |