化学性质
Physical Appearance |
A solid |
Storage |
Store at -20°C |
M.Wt |
564.63 |
Cas No. |
496775-62-3 |
Formula |
C29H36N6O6 |
Synonyms |
Eltrombopag diethanolamine salt;Promacta;Revolade;SB-497115GR |
Solubility |
insoluble in EtOH; insoluble in H2O; ≥14.12 mg/mL in DMSO with gentle warming |
Chemical Name |
2-aminoethanol;3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid |
Canonical SMILES |
CC1=C(C=C(C=C1)N2C(=O)C(=C(N2)C)NN=C3C=CC=C(C3=O)C4=CC(=CC=C4)C(=O)O)C.C(CO)N.C(CO)N |
运输条件 |
蓝冰运输或根据您的需求运输。 |
一般建议 |
为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次半岛bd体育手机客户端 溶解度各有差异,仅做参考。若实验所需浓度过大至半岛bd体育手机客户端 溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
资料参考
Description: IC50 Value: 0.27 uM (EC50 in murine BAF3 cells) [1] Eltrombopag is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis. Potential advantages of eltrombopag may include a sustained platelet response and a good tolerability profile. in vitro: Eltrombopag demonstrated a half maximal effective concentration (EC50) of 0.27 uM in murine BAF3 cells transfected with the luciferase reporter gene under direction of the STAT-activated IRF-1 promoter and human TpoR (BAF3/IRF-1/hTpoR) [1]. Eltrombopag stimulates the growth of TPO-dependent cell lines via JAK2 and STAT signaling pathways and stimulates isolated human CD34+ cells to become megakaryocytes and produce platelets [2]. in vivo: Twelve weeks of antiviral therapy, with concurrent receipt of eltrombopag or placebo, were completed by 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, and 75 mg of eltrombopag, respectively, and by 6% of patients in the placebo group [3]. Eltrombopag was administered as once-daily oral capsules for 10 days at doses of 5, 10, 25, 30, 50, and 75 mg. The pharmacokinetics of eltrombopag was dose dependent and linear, and eltrombopag increased platelet counts in a dose-dependent manner [4]. Toxicity: There were no apparent differences in the incidence or severity of adverse events in subjects receiving active or placebo study medication [4]. Long-term treatment with eltrombopag was generally safe, well tolerated, and effective in maintaining platelet counts in the desired range [5]. Clinical trial: Eltrombopag In Cord Blood Or Haploidentical Bone Marrow Transplantation. Phase 2