1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. HET0016

HET0016 是一种高效、选择性的 20-HETE 合成酶抑制剂,对重组 CYP4A1、CYP4A2 和 CYP4A3 催化 20-HETE 合成作用的 IC50 值分别为 17.7 nM, 12.1 nM 和 20.6 nM。HET0016 是一种选择性 CYP450 抑制剂,已被证明可以抑制血管生成和肿瘤生长。

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HET0016 Chemical Structure

HET0016 Chemical Structure

CAS No. : 339068-25-6

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605
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1 mg ¥250
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5 mg ¥550
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10 mg ¥950
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25 mg ¥1900
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50 mg ¥3500
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth[1][2].

IC50 & Target

CYP4

 

体外研究
(In Vitro)

HET0016 is a selective, non-competitive and irreversible inhibitor of CYP4A [1].
HET0016 (100 μM; 24 hours, 48 hours) decreases migration and invasion of breast cancer metastatic cells [2].

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

Cell Proliferation Assay[2]

Cell Line: MDA-MB-231 cells
Concentration: 100 μM
Incubation Time: 24 hours, 48 hours
Result: Decreased migration and invasion of breast cancer metastatic cells
体内研究
(In Vivo)

HET0016 (10 mg/kg/day; i.v.; for 3 weeks) reduces tumor volume and lung metastasis in an immunocompetent breast cancer mouse model[2].
HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice[2].
HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment[2].
HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins[3].

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

Animal Model: 4–5 weeks female Balb/c mice (16-18 g)[2]
Dosage: 10 mg/kg/day
Administration: Intravenously; 5 days a week; for 3 weeks; starting from day 15 of tumor implantation
Result: Reduced tumor volume and lung metastasis.
分子量

206.28

Formula

C12H18N2O

CAS 号
性状

固体

颜色

White to off-white

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: 

DCM 中的溶解度 : 12.5 mg/mL (60.60 mM; 超声助溶)

DMSO 中的溶解度 : 5 mg/mL (24.24 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.8478 mL 24.2389 mL 48.4778 mL
5 mM 0.9696 mL 4.8478 mL 9.6956 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

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: 20% HP-β-CD in Saline

    Solubility: 2 mg/mL (9.70 mM); 澄清溶液; 超声助溶

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
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 / DCM 1 mM 4.8478 mL 24.2389 mL 48.4778 mL 121.1945 mL
5 mM 0.9696 mL 4.8478 mL 9.6956 mL 24.2389 mL
10 mM 0.4848 mL 2.4239 mL 4.8478 mL 12.1194 mL
15 mM 0.3232 mL 1.6159 mL 3.2319 mL 8.0796 mL
20 mM 0.2424 mL 1.2119 mL 2.4239 mL 6.0597 mL
DCM 25 mM 0.1939 mL 0.9696 mL 1.9391 mL 4.8478 mL
30 mM 0.1616 mL 0.8080 mL 1.6159 mL 4.0398 mL
40 mM 0.1212 mL 0.6060 mL 1.2119 mL 3.0299 mL
50 mM 0.0970 mL 0.4848 mL 0.9696 mL 2.4239 mL
60 mM 0.0808 mL 0.4040 mL 0.8080 mL 2.0199 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:
HET0016
目录号:
HY-124527
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