PARP1-IN-5 dihydrochloride|西域试剂

PARP1-IN-5 dihydrochloride,97.21%

产品编号：Bellancom-132297A| 分子式：C₂₅H₂₆Cl₂N₂O₅S| 分子量：537.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-132297A	￥2500.00	杭州北京（现货）
Bellancom-132297A	￥3800.00	杭州北京（现货）
Bellancom-132297A	￥7500.00	杭州北京（现货）
Bellancom-132297A	￥10500.00	杭州北京（现货）
Bellancom-132297A	￥14500.00	杭州北京（现货）

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PARP1-IN-5 dihydrochloride

产品介绍

PARP1-IN-5 dihydrochloride 是一种低毒、具有口服活性、有效的和有选择性的 PARP-1 抑制剂(IC₅₀ =14.7 nM)。PARP1-IN-5 dihydrochloride 可用于癌症研究。

生物活性

PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC₅₀ =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer.

体外研究

PARP1-IN-5 dihydrochloride (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 dihydrochloride (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 dihydrochloride (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 dihydrochloride (SK-OV-3 cells) can significantly decrease the PAR level.
PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine.
PARP1-IN-5 dihydrochloride (25 and 50 mg/kg; p.o.; 12 days) significantly enhances the inhibitory effect of carboplatin on A549 cells at 50 mg/kg.
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1.
PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice
Dosage:	1000 mg/kg
Administration:	P.o.
Result:	There was no significant difference in the body weight and blood routine.

Animal Model:	Mice
Dosage:	25 and 50 mg/kg
Administration:	P.o.; 12 days
Result:	Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.

Animal Model:	Male Sprague−Dawley (SD) rats
Dosage:	50 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o.
Result:	Positively correlated with the expression of PARP-1.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice
Dosage:	1000 mg/kg
Administration:	P.o.
Result:	There was no significant difference in the body weight and blood routine.

Animal Model:	Mice
Dosage:	25 and 50 mg/kg
Administration:	P.o.; 12 days
Result:	Significantly enhanced the inhibitory effect of CBP on A549 cells at 50 mg/kg.

Animal Model:	Male Sprague−Dawley (SD) rats
Dosage:	50 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o.
Result:	Positively correlated with the expression of PARP-1.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (232.58 mM; Need ultrasonic)

H₂O : 1 mg/mL (1.86 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8606 mL	9.3030 mL	18.6060 mL
5 mM	0.3721 mL	1.8606 mL	3.7212 mL
10 mM	0.1861 mL	0.9303 mL	1.8606 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.87 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。