1. Metabolic Enzyme/Protease Apoptosis
  2. MMP Apoptosis
  3. Prinomastat

Prinomastat  (Synonyms: 普啉司他; AG3340; KB-R9896)

目录号: HY-12170 纯度: 99.27%
COA 产品使用指南

Prinomastat (AG3340) 是一种广谱,有效的口服活性金属蛋白酶 (MMP) 抑制剂,对于 MMP-1, MMP-3MMP-9IC50 分别为 79 nM,6.3 nM 和 5.0 nM。Prinomastat 抑制 MMP-2, MMP-3MMP-13MMP-9Ki 分别为 0.05 nM,0.3 nM,0.03 nM 和 0.26 nM。Prinomastat 穿过血脑屏障。抗肿瘤活性。

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Prinomastat Chemical Structure

Prinomastat Chemical Structure

CAS No. : 192329-42-3

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     可免费申领三个不同产品的试用装。

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1 mg ¥1250
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5 mg ¥3750
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Customer Review

Other Forms of Prinomastat:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3, MMP-13 and MMP-9 with Kis of 0.05 nM, 0.3 nM, 0.03 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity[1][2][3][4].

IC50 & Target[1][3][4]

MMP-9

5 nM (IC50)

MMP-9

0.26 nM (Ki)

MMP-2

0.05 nM (Ki)

MMP-1

79 nM (IC50)

MMP-3

6..3 nM (IC50)

MMP-3

0.3 nM (Ki)

collagenases 3

0.03 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
HL-60 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
HUVEC IC50
> 500 μM
Compound: Prinomastat
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against HUVEC assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
K562 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
KG-1 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human KG1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human KG1 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
MCF7 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
PC-3 IC50
> 500 μM
Compound: Prinomastat
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
[PMID: 31415980]
体外研究
(In Vitro)

Prinomastat (0.1-1 μg/mL;4 天;C57MG/Wnt1 细胞) 抑制 Wnt1 诱导的 MMP-3 产生。通过 Prinomastat 逆转 Wnt1 诱导的 EMT 和 β-catenin 转录活性[1]。将 L/Wnt3a 细胞和 MMP-3 过表达 C57MG 细胞与 CT7 细胞一起培养可使 CT7 细胞中的 Topflash 荧光素酶活性超过 L/Wnt3a 细胞观察到的水平,而这些效应均被 Prinomastat 抑制[1]
Prinomastat 抑制 C57MG/Wnt1 细胞进入 S 期对应于细胞周期蛋白 D1 和 Erk1/2 磷酸化表达的降低。然后使用体外伤口试验检查 Prinomastat 对 Wnt1 诱导的迁移的影响。正如预期的那样,与 C57MG 细胞相比,C57MG/Wnt1 细胞的迁移增加了 1.8 倍。Wnt1 对波形蛋白细胞分布的影响在 C57MG/Wnt1 细胞中被 Prinomastat 逆转[1]

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

Western Blot Analysis[1]

Cell Line: C57MG/Wnt1 cells
Concentration: 0.1 µg/mL, 1 µg/mL
Incubation Time: 4 days
Result: A significant decrease in MMP-3 promoter activity in C57MG/Wnt1 cells.
体内研究
(In Vivo)

在人类纤维肉瘤小鼠模型 (HT1080) 中,从肿瘤接种后的第 3 天到第 6 天开始,每天对小鼠进行 50 mg/kg/天腹腔注射处理,持续 14-16 天。Prinomastat 对动物有很好的耐受性,并且没有体重减轻或其他不良反应的迹象。Prinomastat 具有良好的肿瘤生长抑制作用,T1/2 短至 1.6 小时[1]

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

Clinical Trial
分子量

423.51

Formula

C18H21N3O5S2

CAS 号
性状

固体

颜色

White to off-white

中文名称

普啉司他

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 6 months
-20°C 1 month
溶解性数据
细胞实验: 

H2O 中的溶解度 : 2.5 mg/mL (5.90 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈3))

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3612 mL 11.8061 mL 23.6122 mL
5 mM 0.4722 mL 2.3612 mL 4.7224 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, 6 months; -20°C, 1 month。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 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: 99.27%

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, 6 months; -20°C, 1 month。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 2.3612 mL 11.8061 mL 23.6122 mL 59.0305 mL
5 mM 0.4722 mL 2.3612 mL 4.7224 mL 11.8061 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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:
Prinomastat
目录号:
HY-12170
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