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产品描述： UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research |
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靶点：
IC50: 4.3 nM (Mer), 360 nM (Axl), 250 nM (Tyro);TAMReceptor |
体内研究：
UNC2881 (3 mg/kg; p.o.; single dose) has high systemic clearance (94.5 mL/min/kg) and 14% oral bioavailability, displays terminal half-life of 0.80 h. UNC2881 (3 mg/kg; i.v.; injected with VSV on days -3, -2, -1, and 0) limits Mertk signaling, and promotes the antiviral immune response, reducing the viral replication of vesicular stomatitis virus (VSV) in infected mice. |
参考文献：
1. Zhang W, et al. Discovery of Mer specific tyrosine kinase inhibitors for the treatment and prevention of thrombosis. J Med Chem. 2013 Dec 12;56(23):9693-700. 2. Tom Adomati, et al. Dead Cells Induce Innate Anergy Via Mertk after Acute Viral Infection. Cell Reports. 2020. 30(11):3671-3681. |
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溶解性：
DMSO : ≥ 44 mg/mL (94.91 mM) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
2.157 ml |
10.786 ml |
21.571 ml |
| 5 mM |
0.431 ml |
2.157 ml |
4.314 ml |
| 10 mM |
0.216 ml |
1.079 ml |
2.157 ml |
| 50 mM |
0.043 ml |
0.216 ml |
0.431 ml |
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| 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