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- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1493764-08-1
- 规格:
10 mM * 1 mL/5 mg/10 mg/50 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥714.0 |
|---|---|---|---|
| 规格: | 5 mg | 产品价格: | ¥700.0 |
| 规格: | 10 mg | 产品价格: | ¥1200.0 |
| 规格: | 50 mg | 产品价格: | ¥4000.0 |
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UNC2881
CAS No. : 1493764-08-1
MCE 国际站:UNC2881
产品活性:UNC2881 是一种口服有效、特异性的 Mer 激酶抑制剂,可抑制稳定状态的 Mer 激酶磷酸化,IC50 为 22 nM。UNC2881 对 Axl 和 Tyro 也有抑制作用,IC50 分别为 360 nM 和 250 nM。UNC2881 可有效抑制胶原诱导的血小板聚集,可用于血栓病理研究。
研究领域:Anti-infection | Protein Tyrosine Kinase/RTK
作用靶点:VSV | TAM Receptor
In Vitro: UNC2881 (compound 23) (0-1000 nM; 1 h) block ligand-stimulated activation of a chimeric EGFR-MerTK. UNC2881 also inhibits endogenous Mer tyrosine kinase activation in acute lymphoblastic leukemia cells.
UNC2881 (3 μM; 1 h) suppresses platelet aggregation by greater than 25% in human platelet-rich plasma in response to stimulation with fibrillar type I equine collagen.
In Vivo: 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.
Pharmacokinetics of UNC2881 in mice
| Route | Dose (mg/kg) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUClast (ng·h/mL) | CLobs (mL/min) | Vss (L/kg) | F (%) |
| IV | 3 | 0.8 | 2609 | 527 | 94.5 | 1.65 | ||
| PO | 3 | 0.30 | 90.0 | 71.7 | 14 |
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