UPF 1069
目录号: PL08909 纯度: ≥99%
CAS No. :1048371-03-4
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中文名称
UPF 1069
中文别名
5-(2-氧代-2-苯基乙氧基)-1(2H)-异喹啉酮;UPF1069 抑制剂
英文名称
UPF 1069
英文别名
6H-Oxazolo[4,5-g][3]benzazepine, 7,8,9,10-tetrahydro-8-;UPF 1069;5-(2-oxo-2-phenylethoxy)-1(2H)-Isoquinolinone;5-(2-Oxo-2-phenylethoxy)-3,4-dihydroisoquinolin-1(2H)-one;UPF-1069;1(2H)-Isoquinolinone, 5-(2-oxo-2-phenylethoxy)-;5-Phenacyloxy-2H-isoquinolin-1-one;UPF1069;5-(2-Oxo-2-phenylethoxy)isoquinolin-1(2H)-one;AOB5210;HMS3678B17;HMS3414B17;HMS3653L04;BCP27998;BDBM50232347;2785AH;s8038;SW219733-1;J3.659.361J
Cas No.
1048371-03-4
分子式
C17H13NO3
分子量
279.29
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
UPF 1069 是一种 PARP 抑制剂,对 PARP-1 和 PARP-2 的 IC50 值分别为 8 和 0.3 μM。
生物活性
UPF 1069 is a PARP inhibitor, with IC 50 s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively.
性状
Solid
IC50 & Target[1][2]
PARP-2 0.3 μM (IC50) PARP-1 8 μM (IC5
体外研究(In Vitro)
UPF 1069 (Compound 55) is a PARP inhibitor, with IC50s of 8 and 0.3 μM for PARP-1 and PARP-2, respectively. UPF 1069 (1 μM) reduces the residual PARP activity by approximately 80% of PARP-1-deficient fibroblasts, but only slightly inhibits the enzymic activity in wild-type fibroblasts. UPF 1069 (0.1-1 μM) markedly enhances CA1 hippocampal damage. UPF 1069 (10 μM) also exacerbates oxygen-glucose deprivation (OGD) damage in organotypic hippocampal slices. However, UPF 1069 alleviates the damage cuased by OGD in mixed cortical cell cultures, shows a potent neuroprotective activity both at a concentration (1 μM) selectively acting on PARP-2 and at a concentration (10 μM) inhibiting both PARP-1 and PARP-2 activities. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Pellicciari R, et al. On the way to selective PARP-2 inhibitors. Design, synthesis, and preliminary evaluation of a series of isoquinolinone derivatives. ChemMedChem. 2008 Jun;3(6):914-23.
[2]. Moroni F, et al. Selective PARP-2 inhibitors increase apoptosis in hippocampal slices but protect cortical cells in models of post-ischaemic brain damage.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (358.05 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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