PARP1-IN-5 dihydrochloride

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PARP1-IN-5 dihydrochloride  纯度: 97.21%

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。

PARP1-IN-5 dihydrochloride

PARP1-IN-5 dihydrochloride Chemical Structure

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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[1].

IC50 & Target[1]

PARP-1

14.7 nM (IC50)

PARP-2

0.9 μM (IC50)

体外研究
(In Vitro)

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[1].
PARP1-IN-5 dihydrochloride exerts antitumor effects through PARP-1. PARP1-IN-5 dihydrochloride could increase the γ-H2AX expression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

PARP1-IN-5 dihydrochloride (1000 mg/kg; p.o.) shows that there is no significant difference in the body weight and blood routine[1].
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[1].
PARP1-IN-5 dihydrochloride (50 mg/kg; p.o.) positively correlates with the expression of PARP-1[1].
PARP1-IN-5 dihydrochloride can upregulate the expression of γ-H2AX and decrease the expression of PAR[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[1]
Dosage: 1000 mg/kg
Administration: P.o.
Result: There was no significant difference in the body weight and blood routine.
Animal Model: Mice[1]
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[1]
Dosage: 50 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Positively correlated with the expression of PARP-1.

分子量

537.46

Formula

C25H26Cl2N2O5S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Long H, et al. Discovery of Novel Apigenin-Piperazine Hybrids as Potent and Selective Poly (ADP-Ribose) Polymerase-1 (PARP-1) Inhibitors for the Treatment of Cancer. J Med Chem. 2021;64(16):12089-12108.

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