DR2313

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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。

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-1和PARP-2的IC₅₀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 K_iof 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 mg

5 mg

10 mg

1 mM	5.4873 mL	27.4363 mL	54.8727 mL
5 mM	1.0975 mL	5.4873 mL	10.9745 mL
10 mM	0.5487 mL	2.7436 mL	5.4873 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。