PARP1-IN-5

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PARP1-IN-5

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。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

PARP1-IN-5 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 可用于癌症研究。

生物活性

PARP1-IN-5 is a low toxicity, orally active, potent and selectivePARP-1inhibitor (IC₅₀=14.7 nM). PARP1-IN-5 can be used for the research ofcancer^[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 (0.1~10 μM; A549 cells) can significantly increase the cytotoxicity of CBP on A549 cells in a dose-dependent manner. PARP1-IN-5 (0.1~10 μM; SK-OV-3 cells) decreases the expressions of MCM2-7. PARP1-IN-5 (0.1~320 μM; A549 cells) has little cytotoxic effects on A549 cells. PARP1-IN-5 (SK-OV-3 cells) can significantly decrease the PAR level^[1].
PARP1-IN-5 exerts antitumor effects through PARP-1. PARP1-IN-5 could increase the γ-H2AX expression^[1].

体内研究
(In Vivo)

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

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.; 12 days
Result:	Positively correlated with the expression of PARP-1.

分子量

464.53

Formula

C₂₅H₂₄N₂O₅S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.