半岛bd体育手机客户端 说明
生化/生理作用
Sotrastaurin (AEB071) is an orally active, ATP site-targeting, potent and selective protein kinase C (PKC) inhibitor (Ki in nM/isoform = 0.95/α, 0.64/βI, 2.1/δ, 3.2/ε, 1.8/η and 2.2/θ; IC50 = 2.1/α, 2.0/βI, 1.3/δ, 6.2/ε, 6.1/η and 1.0/θ with 10 μM ATP). Sotrastaurin inhibits TCR/CD28-mediated T cell activation in cultures (IC50 = 54 nM by Jurkat IL-2 promoter reporter line) and exhibitsin vivoimmunosuppressive efficacy in rat models of local graft versus host (GvH) reaction and cardiac transplantation (10 and 30 mg/kg p.o. q.d. or b.i.d.).
基本信息
| 经验(实验)分子式 | C25H22N6O2 |
| 分子量 | 438.48 |
| MDL编号 | MFCD16038049 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | faint brown to dark red |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | ?20℃ |
| SMILES string | O=C(NC1=O)C(C2=CNC3=C2C=CC=C3)=C1C4=C5C=CC=CC5=NC(N6CCN(CC6)C)=N4 |
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