1. Cell Cycle/DNA Damage Epigenetics
  2. PARP
  3. Niraparib (R-enantiomer)

Niraparib (R-enantiomer)  (Synonyms: MK 4827 (R-enantiomer))

目录号: HY-10619D 纯度: 99.69%
COA 产品使用指南 技术支持

Niraparib R-enantiomer (MK-4827 R-enantiomer) 是一种高效的 PARP1 抑制剂,IC50 为 2.4 nM。

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Niraparib (R-enantiomer) Chemical Structure

Niraparib (R-enantiomer) Chemical Structure

CAS No. : 1038915-58-0

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10 mM * 1 mL in DMSO ¥943
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1 mg ¥493
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5 mg ¥1338
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10 mg ¥2038
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25 mg ¥3338
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50 mg ¥4700
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Customer Review

Other Forms of Niraparib (R-enantiomer):

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Niraparib R-enantiomer (MK-4827 R-enantiomer) is an excellent PARP1 inhibitor with IC50 of 2.4 nM.

IC50 & Target[1]

PARP-1

2.4 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa EC50
30 nM
Compound: 22
Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
Inhibition of PARP in human HeLa cells assessed as inhibition of hydrogen peroxide-induced PARylation by cell-based assay
[PMID: 25761096]
HeLa CC50
470 nM
Compound: 22
Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay
Cytotoxicity against human HeLa cells transfected with BRCA1 shRNA assessed as reduction of cell viability after 5 to 7 days by CellTiter-Blue assay
[PMID: 25761096]
HeLa CC50
470 nM
Compound: 57
Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay
Antiproliferative activity against BRCA1 deficient human HeLa cells after 7 days by cell titer-blue assay
[PMID: 19873981]
HeLa CC50
5700 nM
Compound: 57
Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay
Antiproliferative activity against human HeLa cells expressing wild type BRCA1 after 7 days by cell titer-blue assay
[PMID: 19873981]
体外研究
(In Vitro)

Niraparib的R-对映体(MK-4827的R-对映体)分离后得到Niraparib的R-对映体和S-对映体,两者均显示出对PARP-1的优异抑制作用。Niraparib的R-对映体在大鼠肝微粒体中的体外代谢清除率略低于S-对映体,但在基于细胞的试验中,Niraparib的S-对映体表现出更高的效力(PARylation EC50:Niraparib R-对映体=30 nM,Niraparib S-对映体=4.0 nM;BRCA1-HeLa CC50:Niraparib R-对映体=470 nM,Niraparib S-对映体=34 nM)。鉴于这种增强的效力以及在人肝微粒体(HLM)中相似的体外转化率(HLM Clint:Niraparib R-对映体=4 μL/min/mg,Niraparib S-对映体=3 μL/min/mg),研究重点放在了Niraparib的S-对映体(即Niraparib)上[1]

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

分子量

320.39

Formula

C19H20N4O

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 32 mg/mL (99.88 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" 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 3.1212 mL 15.6060 mL 31.2120 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.69%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1212 mL 15.6060 mL 31.2120 mL 78.0299 mL
5 mM 0.6242 mL 3.1212 mL 6.2424 mL 15.6060 mL
10 mM 0.3121 mL 1.5606 mL 3.1212 mL 7.8030 mL
15 mM 0.2081 mL 1.0404 mL 2.0808 mL 5.2020 mL
20 mM 0.1561 mL 0.7803 mL 1.5606 mL 3.9015 mL
25 mM 0.1248 mL 0.6242 mL 1.2485 mL 3.1212 mL
30 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
40 mM 0.0780 mL 0.3901 mL 0.7803 mL 1.9507 mL
50 mM 0.0624 mL 0.3121 mL 0.6242 mL 1.5606 mL
60 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
80 mM 0.0390 mL 0.1951 mL 0.3901 mL 0.9754 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Niraparib (R-enantiomer)
目录号:
HY-10619D
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