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3,5,7,8-四氢-2-甲基-4H-硫代吡喃并[4,3-D]嘧啶-4-酮 /DR2313 {[allProObj[0].p_purity_real_show]}

货号:A336764 同义名: PARP Inhibitor XI

DR2313是一种 PARP 抑制剂,具有显著的抗癌效果,通过抑制 DNA 修复机制来治疗肿瘤。

DR2313 化学结构 CAS号:284028-90-6
DR2313 化学结构
CAS号:284028-90-6
DR2313 3D分子结构
CAS号:284028-90-6
DR2313 化学结构 CAS号:284028-90-6
DR2313 3D分子结构 CAS号:284028-90-6
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DR2313 纯度/质量文件 产品仅供科研

货号:A336764 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PARP PARP1 PARP2 PARP3 其他靶点 纯度
PJ34 HCl ++

PARP, EC50: 20 nM

99%+
Rucaparib phosphate ++++

PARP, Ki: 1.4 nM

99%+
3-Aminobenzamide ++

PARP, IC50: <50 nM

98%
AZD-2461 99%+
BGP-15 99%+
NU1025 +

PARP, IC50: 400 nM

97%
Benzamide +

PARP, IC50: 3.3 μM

98%
Picolinamide +

PARP, IC50: 95 μM

98%
AG14361 +++

PARP1, Ki: <5 nM

98+%
Iniparib 98%
Talazoparib ++++

PARP1, IC50: 0.57 nM

99%+
NMS-P118 ++

PARP1, Kd: 0.009 μM

98+%
UPF 1069 +

PARP1, IC50: 8.0 μM

++

PARP2, IC50: 0.3 μM

98%
A-966492 ++++

PARP1, EC50: 1 nM

PARP1, Ki: 1 nM

+++

PARP2, Ki: 1.5 nM

99%+
Veliparib ++

PARP1, Ki: 5.2 nM

+++

PARP2, Ki: 2.9 nM

98%
Niraparib tosylate +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

99%+
Stenoparib ++++

PARP1, IC50: 1 nM

++++

PARP2, IC50: 1.2 nM

98%
Olaparib +++

PARP1, IC50: 5 nM

++++

PARP2, IC50: 1 nM

98%
Niraparib +++

PARP1, IC50: 3.8 nM

+++

PARP2, IC50: 2.1 nM

98%
ME0328 +

PARP1, IC50: 6.3 μM

+

PARP3, IC50: 0.89 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

DR2313 生物活性

描述 DR2313 is a potent, selective, competitive and brain-penetrating PARP inhibitor with IC50 values of 0.20 μM for PARP-1 and 0.24 μM for PARP-2. DR2313 is neuroprotective against ischaemic injury in vitro and in vivo[1][2].In the concentration range of 0.016-16.4 μM, DR2313 can inhibit the poly(ADP-ribosyl)ation reaction in rat brain nuclear extract for 30 minutes, with a Ki of 0.23 μM. In the concentration range of 1-100 μM, DR2313 showed a weak inhibitory effect on mono(ADP-ribosyl)ation in a concentration-dependent manner for 10 minutes, with an IC50 value of 59 μM. DR2313 reduces hydrogen peroxide (500 μM; 4 hours) or glutamate (1 mM; 30 minutes)-induced poly(ADP-ribose) and cell death in the concentration range of 0.1-30 μM and 30 minutes of pretreatment[1] .

DR2313 动物研究

Animal study DR2313 significantly reduced cortical infarct volume in a rat model of permanent and transient focal ischaemia at doses of 3-10 mg/kg administered intravenously or by infusion over 6 hours[1].

DR2313 参考文献

[1]Nakajima H, et, al. A newly synthesized poly(ADP-ribose) polymerase inhibitor, DR2313 [2-methyl-3,5,7,8-tetrahydrothiopyrano[4,3-d]-pyrimidine-4-one]: pharmacological profiles, neuroprotective effects, and therapeutic time window in cerebral ischemia in r

[2]Xu Z, et, al. Endonuclease G does not play an obligatory role in poly(ADP-ribose) polymerase-dependent cell death after transient focal cerebral ischemia. Am J Physiol Regul Integr Comp Physiol. 2010 Jul;299(1):R215-21.

DR2313 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

5.49mL

1.10mL

0.55mL

27.44mL

5.49mL

2.74mL

54.87mL

10.97mL

5.49mL

DR2313 技术信息

CAS号284028-90-6
分子式C8H10N2OS
分子量 182.243
别名 PARP Inhibitor XI
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解度

DMSO: 12 mg/mL(65.85 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 100 mg/mL(548.72 mM)

动物实验配方
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