Diroleuton

二高-γ-亚麻酸可以抑制人和小鼠巨噬细胞中促炎基因的表达[2]。二高-γ-亚麻酸（50 μM；24 小时）可减弱 IFN-γ 诱导的 STAT1 丝氨酸 727 磷酸化 [2]。当IL-1β和TNF-α释放到人巨噬细胞中时，二高-γ-亚麻酸可以降低MCP-1和ICAM-1的表达[2]。二高-γ-亚麻酸抑制趋化因子诱导的单核细胞迁移和巨噬细胞泡沫细胞形成[2]。二高-γ-亚麻酸可减弱人巨噬细胞中 CD36 和 SR-A 的表达 [2]。二高-γ-亚麻酸控制线粒体的呼吸[2]。二高-γ-亚麻酸影响 VSMC 和内皮细胞的行为 [2]。

在患有小异种移植肿瘤的小鼠中，diho-γ-亚麻酸（8 毫克/小鼠；每周注射两次，持续 35 天）可抑制转染 delta-5-去饱和酶 shRNA 的人胰腺癌细胞 (BxPC-3) 的发育 [3] 。

蛋白质印迹分析 [2]
细胞类型： THP-1 巨噬细胞
测试浓度： 50 μM（预处理）
孵育时间： 24 小时
实验结果： IFN-γ 诱导的 STAT1 丝氨酸 727 磷酸化减弱。

Animal/Disease Models: Female nude mice (48, four weeks old) [3]
Doses: 8 mg/animal
Route of Administration: po (oral gavage), twice a week for 35 days
Experimental Results: Inhibited the metastasis potential of D5D-KD tumors.

[1]. Multiple roles of dihomo-γ-linolenic acid against proliferation diseases. Lipids Health Dis. 2012 Feb 14;11:25.

[2]. Dihomo-γ-linolenic acid inhibits several key cellular processes associated with atherosclerosis. Biochim Biophys Acta Mol Basis Dis. 2019 Sep 1;1865(9):2538-2550.

[3]. Dihomo-γ-linolenic acid inhibits growth of xenograft tumors in mice bearing human pancreatic cancer cells (BxPC-3) transfected with delta-5-desaturase shRNA. Redox Biol. 2019 Jan;20:236-246.

All-cis-icosa-8,11,14-trienoic acid is an icosatrienoic acid having three cis double bonds at positions 8, 11 and 14. It has a role as a nutraceutical, a human metabolite and a fungal metabolite. It is a fatty acid 20:3 and a long-chain fatty acid. It is a conjugate acid of an all-cis-icosa-8,11,14-trienoate.
A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.
Dihomo-gamma-linolenic acid has been reported in Mortierella hygrophila, Mortierella alpina, and other organisms with data available.
Dihomo-gamma-linolenic Acid is a polyunsaturated long-chain fatty acid with a 20-carbon backbone and 3 double bonds, originating from the 6th, 9th and 12th positions from the methyl end, with all bonds in the cis- configuration.
A 20-carbon-chain fatty acid, unsaturated at positions 8, 11, and 14. It differs from arachidonic acid, 5,8,11,14-eicosatetraenoic acid, only at position 5.

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Drug Indication
For nutritional supplementation, also for treating dietary shortage or imbalance

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Mechanism of Action
DHLA (or DGLA) is a precursor in the synthesis of prostaglandin E1 (PGE1) as well as the series-3 prostaglandins. It also serves as a precursor in the synthesis of eicosapentaenoic acid (EPA). EPA is a precursor of the series-3 prostaglandins, the series-5 leukotrienes and the series-3 thromboxanes. These eicosanoids have anti-thrombogenic, anti-inflammatory and anti-atherogenic properties. PGE1 inhibits platelet aggregation and has a vasodilation action. DHLA has also been shown to reduce the production/activity of tumor necrosis factor alpha.

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Pharmacodynamics
Dihomo gamma-linolenic acid or DHLA is an n-6 (omega-6) polyunsaturated fatty acid. It is comprised of 20 carbon atoms and three double bonds. DHLA is a byproduct of the 18 carbon gamma-linolenic acid (GLA). DHLA is then converted into prostaglandin E1 (PGE1). PGE1 inhibits platelet aggregation and also exerts a vasodilatory effect.

C20H34O2

306.4828

306.255

1783-84-2

5280581

Colorless to light yellow liquid

0.917g/cm3

437.984°C at 760 mmHg

334.667°C

0.0±2.3 mmHg at 25°C

1.489

7.56

37.3

1

2

15

22

327

0

O([H])C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])/C(/[H])=C(/[H])\C([H])([H])/C(/[H])=C(/[H])\C([H])([H])/C(/[H])=C(/[H])\C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])=O

HOBAELRKJCKHQD-QNEBEIHSSA-N

InChI=1S/C20H34O2/c1-2-3-4-5-6-7-8-9-10-11-12-13-14-15-16-17-18-19-20(21)22/h6-7,9-10,12-13H,2-5,8,11,14-19H2,1H3,(H,21,22)/b7-6-,10-9-,13-12-

(8Z,11Z,14Z)-icosa-8,11,14-trienoic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~326.29 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (8.16 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中，混匀；然后向上述溶液中加入50 μL Tween-80，混匀；加入450 μL生理盐水定容至1 mL。
*生理盐水的制备：将 0.9 g 氯化钠溶解在 100 mL ddH₂O中，得到澄清溶液。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (8.16 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液。
例如，若需制备1 mL的工作液，可将 100 μL 25.0 mg/mL 澄清 DMSO 储备液加入到 900 μL 玉米油中并混合均匀。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。