OUL232

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OUL232

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:

943119-42-4

OUL232 是单ARTs PARP7、PARP10、PARP11、PARP12、PARP14和PARP15的有效抑制剂。OUL232 是迄今为止描述的最有效的PARP10抑制剂 (IC₅₀=7.8 nM)，也是报道的第一个PARP12抑制剂。

生物活性

OUL232 is a potent inhibitor ofmono-ARTsPARP7,PARP10, PARP11, PARP12,PARP14,andPARP15. OUL232 is the most potentPARP10inhibitor described to date (IC₅₀=7.8 nM), as well as the firstPARP12inhibitor ever reported^[1].

IC₅₀& Target^[1]

PARP7

83 nM (IC₅₀)

PARP10

7.8 nM (IC₅₀)

PARP14

300 nM (IC₅₀)

PARP15

56 nM (IC₅₀)

PARP1

15 μM (IC₅₀)

PARP2

10 μM (IC₅₀)

PARP3

50 μM (IC₅₀)

PARP4

11 μM (IC₅₀)

TNKS1

5.4 μM (IC₅₀)

TNKS2

10 μM (IC₅₀)

PARP11

240 nM (IC₅₀)

PARP12

160 nM (IC₅₀)

PARP16

3.4 μM (IC₅₀)

体外研究
(In Vitro)

OUL232 (化合物 27) (1 μM; 10-12 d) 拯救过表达 PARP10 的细胞，使其免于 ADP 核糖化依赖的细胞死亡^[1]。

药代动力学分析^[1]

water solubility μg/mL	GIP_app×10^-6cm/s (RM %)	BBBP_app×10^-6cm/s (RM %)	metabolic stablity %	stab in human plasma	stab. in MeOH	stab in PBS pH 7.4
12.60	0.144	0.143	99.11	>24	>24	>24

分子量

250.28

Formula

C₁₀H₁₀N₄O₂S

CAS 号

943119-42-4

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.