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DR2313
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DR2313图片
CAS NO:284028-90-6
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
DR2313 是一种有效,选择性,竞争性的和可透过血脑屏障的PARP抑制剂,抑制PARP-1PARP-2IC50值分别为 0.20 μM 和 0.24 μM。DR2313 在体外和体内均表现出对缺血性损伤的神经保护作用。
生物活性

DR2313 is a potent, selective, competitive and brain-penetrant inhibitor ofpoly(ADP-ribose) polymerase (PARP), withIC50s of 0.20 μM and 0.24 μM forPARP-1andPARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo[1][2].

IC50& Target[1]

PARP-1

0.20 μM (IC50)

PARP-2

0.24 μM (IC50)

体外研究
(In Vitro)

DR2313 (0.016-16.4 μM; 30 min) inhibits poly(ADP-ribosyl)ation reaction in nuclear extracts of rat brain, with a Kiof 0.23 μM[1].
DR2313 shows more powerful inhibition of the poly(ADP-ribosyl)ation in the nuclear extracts of the rat brain (IC50=0.20 μM) than 3AB (35.4 μM), PND (0.56 μM), DIQ (2.96 μM), and DPQ (0.96 μM)[1].
DR2313 (1-100 μM; 10 min) shows a weak inhibition of the mono(ADP-ribosyl)ation in a concentration-dependent manner (IC50=59 μM)[1].
DR2313 (0.1-30 μM; pretreated for 30 min) reduces hydrogen peroxide (500 μM; 4 h) or glutamate (1 mM; 30 min) induced excessive formation of poly(ADP-ribose) and cell death[1].

体内研究
(In Vivo)

DR2313 (3-10 mg/kg i.v. bolus or infusion for 6 h) significantly reduces the cortical infarct volume in both permanent and transient focal ischemia models in rats[1].

Animal Model:Male Wistar rats (220-300 g) with permanent MCA occlusions (pMCAos) and transient MCA occlusions (tMCAos)[1]
Dosage:3, 10 mg/kg
Administration:I.v. bolus and i.v. infusion for 6 h beginning 5 min before the onset of ischemia
Result:Reduced the infarct volume in a dose-dependent manner in pMCAo and tMCAo model.
分子量

182.24

性状

Solid

Formula

C8H10N2OS

CAS 号

284028-90-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

H2O : ≥ 100 mg/mL(548.73 mM)

DMSO : 12.5 mg/mL(68.59 mM;Need ultrasonic)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM5.4873 mL27.4363 mL54.8727 mL
5 mM1.0975 mL5.4873 mL10.9745 mL
10 mM0.5487 mL2.7436 mL5.4873 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。