Vasodilator

前列地尔增加了LPS刺激的H9c2细胞的细胞活力，减少了LDH和肌钙蛋白的产生，并减弱了IL-1β、IL-6、IL-17和TNF-α的分泌。此外，前列地尔降低了LPS处理的H9c2细胞中Wnt5a、JNK和NF-κB的mRNA表达，并降低了Wnt5a，NF-κB的表达以及p-JNK/JNK的比值。siWnt5a或JNK抑制剂SP600125显著增强了前列地尔对Wnt5a/JNK/NF-κB通路的抑制作用[1]。

与Sham组相比，CLP组大鼠血清肝功能标志物含量显著升高，凋亡肝细胞增加，氧化应激水平上调，TLR4/NF-κB通路活性增强，TNF-α释放增加（p<0.05）。同时，CLP组与Sham组相比，显微镜检查有明显的病理变化（p<0.05）。与CLP组相比，Alp组表现出肝功能标志物浓度显著降低，显微镜下发现，如间质炎性细胞浸润减少，凋亡细胞比例显著降低，氧化应激水平降低，TLR4/NF-κB通路活性减弱，TNF-α释放受到抑制（p<0.05）。此外，与CLP组相比，Alp组的肝细胞形态正常（p<0.05）[2]。

在倒置光学显微镜下观察细胞形态，同时用3-（4,5-二甲基噻唑基-2）-2,5-二苯基溴化四唑（MTT）法评估细胞存活率。酶联免疫吸附试验（ELISA）用于研究细胞损伤的生化指标，如释放的乳酸脱氢酶（LDH）和肌钙蛋白，以及炎性细胞因子水平，包括白细胞介素-1β（IL-1β）、IL-6、IL-17和肿瘤坏死因子-α（TNF-α）。通过实时定量聚合酶链式反应（RT-PCR）进一步研究了Wnt5a、c-jun N末端激酶（JNK）和核因子κB（NF-κB）的mRNA表达水平。通过蛋白质印迹法检测前列地尔对H9c2细胞中Wnt5a/JNK/NF-κB通路的影响[1]。

Objective: The aim of this study was to explore the role of alprostadil (Alp) in cecal ligation and puncture (CLP)-induced septic injury in rats and its possible mechanism of action.[2]
Materials and methods: Wistar rats were randomly assigned into three groups, including: Sham group (no CLP was performed), CLP group (CLP was conducted) and Alp group (Alp was injected after CLP). Serum liver function markers, pathological changes in liver tissues, alterations in the level of oxidative stress, activity of the Toll-like receptor 4 (TLR4)/nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway, and release of inflammatory factor tumor necrosis factor alpha (TNF-α) in the liver tissue homogenate were detected in each group.[2]

[1].Alprostadil attenuates LPS-induced cardiomyocyte injury by inhibiting the Wnt5a/JNK/NF-κB pathway. Herz. 2020; 45(Suppl 1): 130–138.
[2]. Alprostadil alleviates liver injury in septic rats via TLR4/NF-κB pathway. https://pubmed.ncbi.nlm.nih.gov/33629328/
[3]. Stability of Alprostadil in 0.9% Sodium Chloride Stored in Polyvinyl Chloride Containers. Int J Pharm Compd. 2017 Mar-Apr;21(2):150-153.

The stability of alprostadil diluted in 0.9% sodium chloride stored in polyvinyl chloride (VIAFLEX) containers at refrigerated temperature, protected from light, is reported. Five solutions of alprostadil 11 mcg/mL were prepared in 250 mL 0.9% sodium chloride polyvinyl chloride (PL146) containers. The final concentration of alcohol was 2%. Samples were stored under refrigeration (2°C to 8°C) with protection from light. Two containers were submitted for potency testing and analyzed in duplicate with the stability-indicating high-performance liquid chromatography assay at specific time points over 14 days. Three containers were submitted for pH and visual testing at specific time points over 14 days. Stability was defined as retention of 90% to 110% of initial alprostadil concentration, with maintenance of the original clear, colorless, and visually particulate-free solution. Study results reported retention of 90% to 110% initial alprostadil concentration at all time points through day 10. One sample exceeded 110% potency at day 14. pH values did not change appreciably over the 14 days. There were no color changes or particle formation detected in the solutions over the study period. This study concluded that during refrigerated, light-protected storage in polyvinyl chloride (VIAFLEX) containers, a commercial alcohol-containing alprostadil formulation diluted to 11 mcg/mL with 0.9% sodium chloride 250 mL was stable for 10 days.[3]

C22H38O5

382.53412

382.271

C, 69.08; H, 10.01; O, 20.91

35900-16-4

745-65-3 (free acid); 217182-28-0 (isopropyl ester); 27930-45-6 (sodium); 35900-16-4 (ethyl ester)

9800148

Typically exists as solid at room temperature

1.1±0.1 g/cm3

498.6±45.0 °C at 760 mmHg

160.9±22.2 °C

0.0±2.9 mmHg at 25°C

1.524

3.24

83.83

2

5

15

27

460

4

CCCCC[C@@H](/C=C/[C@@H]1[C@@H](CCCCCCC(=O)OCC)C(=O)C[C@H]1O)O

LVDCZROIKIHUKJ-QZCLESEGSA-N

1S/C22H38O5/c1-3-5-8-11-17(23)14-15-19-18(20(24)16-21(19)25)12-9-6-7-10-13-22(26)27-4-2/h14-15,17-19,21,23,25H,3-13,16H2,1-2H3/b15-14+/t17-,18+,19+,21+/m0/s1

Prost-13-en-1-oic acid, 11,15-dihydroxy-9-oxo-, ethyl ester, (11alpha,13E,15S)-

Prostaglandin E1 ethyl ester; 35900-16-4; PGE1 ethyl ester; IG6WR57RZT; Prost-13-en-1-oic acid, 11,15-dihydroxy-9-oxo-, ethyl ester, (11alpha,13E,15S)-; ethyl 7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]heptanoate; UNII-IG6WR57RZT;

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)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。