| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Alprostadil ethyl ester is an esterified form and ethyl ester analog of prostaglandin E1 (PGE1) that can be used in the treatment of scleroderma.
| Targets |
Vasodilator
|
|---|---|
| ln Vitro |
Alprostadil increased the cell viability of LPS-stimulated H9c2 cells, reduced LDH and troponin production, and attenuated IL-1β, IL-6, IL-17, and TNF-α secretion. Moreover, alprostadil reduced the mRNA expression of Wnt5a, JNK, and NF-κB and decreased the expression of Wnt5a, NF-κB, and the ratio of p‑JNK/JNK in H9c2 cells treated with LPS. The siWnt5a or JNK inhibitor SP600125 significantly augmented the inhibitory effects of alprostadil on the Wnt5a/JNK/NF-κB pathway[1].
|
| ln Vivo |
Compared with Sham group, the rats in CLP group had substantially elevated content of serum liver function markers, increased apoptotic liver cells, upregulated levels of oxidative stress, enhanced activity of the TLR4/NF-κB pathway, and increased release of TNF-α (p<0.05). Meanwhile, there were evident pathological changes under microscopic examination in CLP group compared with Sham group (p<0.05). In comparison with CLP group, Alp group exhibited significantly decreased concentrations of liver function markers, microscopic findings, such as decreased inflammatory cell infiltration in the interstitum, notably lowered proportion of apoptotic cells, decreased level of oxidative stress, weakened activity of the TLR4/NF-κB pathway and restrained release of TNF-α (p<0.05). Furthermore, normal morphology of liver cells was observed in Alp group compared with CLP group (p<0.05)[2].
|
| Cell Assay |
Cell morphology was observed under an inverted light microscope, while cell viability was assessed with the 3‑(4,5-dimethylthiazolyl-2)-2,5-diphenyltetrazolium bromide (MTT) assay. Enzyme-linked immunosorbent assays (ELISA) were conducted to study biochemical indicators of cellular damage, such as released lactate dehydrase (LDH) and troponin, and inflammatory cytokine levels including interleukin-1β (IL-1β), IL-6, IL-17, and tumor necrosis factor-α (TNF-α). The mRNA expression levels of Wnt5a, c‑jun N‑terminal kinase (JNK), and nuclear factor kappa B (NF-κB) were further investigated by real-time quantitative polymerase chain reaction (RT-PCR). The effects of alprostadil on the Wnt5a/JNK/NF-κB pathway in H9c2 cells was examined by Western blotting[1].
|
| Animal Protocol |
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] |
| References |
[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. |
| Additional Infomation |
This article reports the stability of apratropium tadil solutions diluted with 0.9% sodium chloride in PVC (VIAFLEX) containers under light-protected and refrigerated conditions. Five aliquots of apratropium tadil solutions with a concentration of 11 mcg/mL were prepared and placed in 250 mL PVC (PL146) containers containing 0.9% sodium chloride. The final alcohol concentration was 2%. Samples were stored under light-protected and refrigerated conditions (2°C to 8°C). Two samples were used for potency testing, and repeated analyses were performed at specific time points within 14 days using stability-indicating high-performance liquid chromatography (HPLC). Three other samples were used for pH and appearance testing at specific time points within 14 days. Stability was defined as the apratropium tadil concentration remaining at 90% to 110% of the initial concentration, with the solution remaining clear, colorless, and free of particulate matter. The results showed that the initial concentration of apratropium tadil remained at 90% to 110% at all time points up to day 10. One of the samples had a potency exceeding 110% on day 14. The pH value did not change significantly within 14 days. No color change or particle formation was detected in the solution during the study. The study concluded that a commercially available alcohol-containing prostaglandin E1 formulation (250 mL) diluted to 11 mcg/mL with 0.9% sodium chloride solution could be stably stored for 10 days when refrigerated and protected from light in a VIAFLEX container. [3]
|
| Molecular Formula |
C22H38O5
|
|---|---|
| Molecular Weight |
382.53412
|
| Exact Mass |
382.271
|
| Elemental Analysis |
C, 69.08; H, 10.01; O, 20.91
|
| CAS # |
35900-16-4
|
| Related CAS # |
745-65-3 (free acid); 217182-28-0 (isopropyl ester); 27930-45-6 (sodium); 35900-16-4 (ethyl ester)
|
| PubChem CID |
9800148
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
498.6±45.0 °C at 760 mmHg
|
| Flash Point |
160.9±22.2 °C
|
| Vapour Pressure |
0.0±2.9 mmHg at 25°C
|
| Index of Refraction |
1.524
|
| LogP |
3.24
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
15
|
| Heavy Atom Count |
27
|
| Complexity |
460
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
CCCCC[C@@H](/C=C/[C@@H]1[C@@H](CCCCCCC(=O)OCC)C(=O)C[C@H]1O)O
|
| InChi Key |
LVDCZROIKIHUKJ-QZCLESEGSA-N
|
| InChi Code |
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
|
| Chemical Name |
Prost-13-en-1-oic acid, 11,15-dihydroxy-9-oxo-, ethyl ester, (11alpha,13E,15S)-
|
| Synonyms |
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;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
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
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6142 mL | 13.0709 mL | 26.1417 mL | |
| 5 mM | 0.5228 mL | 2.6142 mL | 5.2283 mL | |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6142 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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