17-ODYA
(Synonyms: 17-十八炔酸,Alk-16) 目录号 : GC12757
17-ODYA是一种非选择性抑制剂，通过细胞色素P450抑制花生四烯酸的ω-羟基化和环氧化作用（IC50<100nM）。
Cas No.:34450-18-5
Sample solution is provided at 25 µL, 10mM.
17-ODYA, a non-selective inhibitor of both ω-hydroxylation and epoxygenation of arachidonic acid via cytochrome P450 (IC50<100nM). 17-ODYA effectively suppressed the production of 20-hydroxyeicosatetraenoic acid, epoxyeicosatrienoic acids, and dihydroxyeicosatrienoic acids by rat renal cortical microsomes when exposed to arachidonic acid[1,2].
17-ODYA as the highest unique metabolite in periapical abscesses, acts an essential role in the Pathogenesis of Periapical Abscesses, one of the most frequent pathologic lesions in the alveolar bone. 17-ODYA caused significant up-regulation of interleukin-1α, interleukin-1β, interleukin-6, matrix metalloproteinase-1, monocyte chemoattractant protein-1 and platelet-derived growth factor alpha and vascular endothelial growth factor alpha at 10μmol/L in periodontal ligament fibroblasts.1μmol/L 17-ODYA caused the same effect in peripheral blood mononuclear cells. These affected cytokines have important biological activities in coordinating the body's response to infection[3].
17-ODYA delivered via the superfusate for 45mins at 10mmol/l, inhibits both local and conducted responses of microiontophoresis of ACh evoked vasodilation that conducted along arterioles in C57Bl6 mice[4].
References:
[1] Zou A P, Ma Y H, Sui Z H, et al. Effects of 17-octadecynoic acid, a suicide-substrate inhibitor of cytochrome P450 fatty acid omega-hydroxylase, on renal function in rats[J]. Journal of Pharmacology and Experimental Therapeutics, 1994, 268(1): 474-481.
[2] Manicam C, Ginter N, Li H, et al. Compensatory vasodilator mechanisms in the ophthalmic artery of endothelial nitric oxide synthase gene knockout mice[J]. Scientific reports, 2017, 7(1): 7111.
[3] Altaie A M, Mohammad M G, Madkour M I, et al. The essential role of 17-octadecynoic acid in the pathogenesis of periapical abscesses[J]. Journal of Endodontics, 2023, 49(2): 169-177. e3.
[4] Hnngerford J E, Sessa W C, Segal S S. Vasomotor control in arterioles of the mouse cremaster muscle[J]. The FASEB journal, 2000, 14(1): 197-207.
17-ODYA是一种非选择性抑制剂，通过细胞色素P450抑制花生四烯酸的ω-羟基化和环氧化作用（IC50<100nM）。当花生四烯酸暴露于大鼠肾皮质微粒体时，17-ODYA有效地抑制了20-羟基二十碳四烯酸、环氧二十碳三烯酸和二羟基二十碳三烯酸的产生[1,2]。
17-ODYA 是根尖周脓肿中含量最高的独特代谢物，在根尖周脓肿的发病机制中起着至关重要的作用，根尖周脓肿是牙槽骨中最常见的病变之一。 在牙周韧带成纤维细胞中，当浓度为 10μmol/L 时，17-ODYA 会显著上调 白介素-1α、白介素-1β、白介素-6、基质金属蛋白酶-1、单核细胞趋化蛋白-1、血小板衍生生长因子α和血管内皮生长因子α。这些细胞因子在协调机体对感染的反应方面具有重要的生物活性[3]。
17-ODYA以10mmol/L的浓度经由超滤液注入，连续注入45分钟，可以抑制C57Bl6小鼠沿动脉小分支传导的乙酰胆碱诱导的血管舒张的局部和传导性反应[4]。
| Cell experiment [1]: | |
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Cell lines |
Human neutrophils |
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Preparation Method |
Pre-warmed human neutrophil suspensions (37°C, 5 million cells/ml in HBSS containing 1.6 mM CaCl2) were incubated 5 minutes with vehicle (DMSO), PF-4708671 (30μM, 5 minutes), or 17-ODYA (30μM, 30 minutes), then treated with 1μM of LTB4 for the indicated times. Samples then were processed and analyzed for LTB4 biosynthesis, then performing kinetic experiments in which neutrophils were incubated with 1μM LTB4. |
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Reaction Conditions |
30μM 17-ODYA for 30 minutes |
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Applications |
17-ODYA increased LTB4 half-life by 5 folds, from ~10 sminutes to ~50 minutes. In comparison, PF-4708671 increased the half-life of LTB4 by 7.5 folds, from ~20 minutes to ~150 minutes. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague-Dawley rats (9-12 week old) |
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Preparation Method |
Rats (n=9) were pretreated 30 mins before subarachnoid hemorrhage (SAH) with N-hydroxy-N'-(4-butyl-2-methylphenyl) formamidine (HET0016) (10mg/kg iv) or 17-ODYA (1.5nmol intrathecally) (n=7 each) or vehicle (n=15). An additional control group of rats (n=9) received an infusion of an equal volume of artificial cerebrospinal fluid in the cisterna magna SAH was induced by injecting 0.3 mL of blood into the cisterna magna over a 10-min period. The effects of two inhibitors on the changes on regional cerebral blood flow (rCBF) after induction of SAH were measured with laser-Doppler flowmetry. |
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Dosage form |
1.5nM, 50μL, cisterna magna injection |
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Applications |
Both 17-ODYA and HET0016 attenuated fall in rCBF recorded at 10mins after induction of SAH by 40%, and rCBF completely recovered within 60mins after induction of SAH in rats treated with 17-ODYA and within 90mins in rats treated with HET0016. |
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References: [1] Archambault A S, Turcotte C, Martin C, et al. Leukotriene B₄ Metabolism and p70S6 Kinase 1 Inhibitors: PF-4708671 but Not LY2584702 Inhibits CYP4F3A and the ω-Oxidation of Leukotriene B₄ In Vitro and In Cellulo[J]. Plos one, 2017, 12(1): e0169804. |
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| Cas No. | 34450-18-5 | SDF | |
| 别名 | 17-十八炔酸,Alk-16 | ||
| 化学名 | octadec-17-ynoic acid | ||
| Canonical SMILES | OC(CCCCCCCCCCCCCCCC#C)=O | ||
| 分子式 | C18H32O2 | 分子量 | 280.45 |
| 溶解度 | 1 mg/mL in DMSO, 10mg/mL in DMF,10mg/mL in ethanol | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.5657 mL | 17.8285 mL | 35.657 mL |
| 5 mM | 0.7131 mL | 3.5657 mL | 7.1314 mL |
| 10 mM | 0.3566 mL | 1.7828 mL | 3.5657 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet