| 产品描述： | JAK2 选择性抑制剂;JAK2 Selective Inhibitors;;InformationPF-06700841 (PF-841) is a potent inhibitor ofTyk2andJak1with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.TargetsJAK1 (Cell-free assay); Tyk2 (Cell-free assay); JAK2 (Cell-free assay) 17 nM; 23 nM; 77 nMIn vivoThe pharmacokinetics of PF-06700841 are studied in Sprague−Dawley rats following intravenous and oral administration (1 and 3 mg/kg respectively) of the tosylate salt, where the compound shows a plasma clearance of 31 mL/min/kg, a volume of distribution of 2.0 L/kg, and oral bioavailability of 83%. Following the 3 mg/kg oral dose, the Cmax is 774 ng/mL and the AUC∞ is 1340 ng·h/mL. The high oral bioavailability indicates high absorption from the gut, consistent with its in vitro passive permeability properties and high solubility. |
| 体内研究： |
Brepocitinib (PF-06700841; Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM. |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.568 ml |
12.84 ml |
25.681 ml |
| 5 mM |
0.514 ml |
2.568 ml |
5.136 ml |
| 10 mM |
0.257 ml |
1.284 ml |
2.568 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.514 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京