HET0016|cas:339068-25-6|西域试剂

HET0016,99.77%

产品编号：Bellancom-124527| CAS NO：339068-25-6| 分子式：C₁₂H₁₈N₂O| 分子量：206.28

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货号	价格	库存与货期
Bellancom-124527	￥550.00	杭州北京（现货）
Bellancom-124527	￥950.00	杭州北京（现货）
Bellancom-124527	￥1900.00	杭州北京（现货）
Bellancom-124527	￥3500.00	杭州北京（现货）
Bellancom-124527	￥6500.00	杭州北京（现货）

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HET0016

产品介绍

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。

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.

体外研究

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

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

Cell Proliferation Assay

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.
HET0016 reduces the metalloproteinases’ levels in the lungs via PI3K/AKT pathway in mice.
HET0016 decreases expression of pro-inflammatory and growth factors and granulocytic MDSCs population in lung microenvironment.
HET0016 protects BBB dysfunction after I/R by regulating the expression of MMP-9 and tight junction proteins.

西域 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)
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.

体内研究

西域 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)
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.

体内研究

西域 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)
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.

性状

Solid

溶解性数据

In Vitro:

DCM : 12.5 mg/mL (60.60 mM; Need ultrasonic)

DMSO : 5 mg/mL (24.24 mM; Need ultrasonic)

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
10 mM	0.4848 mL	2.4239 mL	4.8478 mL

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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；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