S87683 |
BYK204165 |
源叶(MedMol) | 98% |
- 产品描述: BYK204165 is a potent and selective PARP1 inhibitor. BYK204165 inhibits cell-free recombinant human PARP-1 (hPARP-1) with a pIC50 of 7.35 (pKi=7.05), and murine PARP-2 (mPARP-2) with a pIC50 of 5.38, respectively. BYK204165 displays 100-fold selectivity for PARP-1
- 靶点: hPARP-1:7.35 (pIC50);mPARP-2:5.38 (pIC50);PARP
- 体外研究:
In kinetic experiments with human PARP-1, BYK204165 exhibits potent and competitive inhibition of enzyme activity, yielding a pKi value of 7.05[1].BYK204165 exhibits low potency of PARP inhibition in C4I cells (pIC50 of 5.75)
- 体内研究:
BYK204165 is not investigated in vivo because of its short half-time (t1/2) of 23 min measured at rat microsomes in vitro
- 参考文献:
1. Eltze T, et al. Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. Mol Pharmacol. 2008 Dec;74(6):1587-98.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.964 ml 19.82 ml 39.64 ml 5 mM 0.793 ml 3.964 ml 7.928 ml 10 mM 0.396 ml 1.982 ml 3.964 ml 50 mM 0.079 ml 0.396 ml 0.793 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。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)