Iloprost
Based on 5 publication(s) in Google Scholar
Iloprost (ZK 36374; Ciloprost) is a prostacyclin (PGI2) analogue, involves in embryo development and inflammation improvement, and inhibits tumor metastasis. Iloprost can be used for peripheral vascular research.
For research use only. We do not sell to patients.
- Purity: 98.32%
- CAS No.: 78919-13-8
- Formula: C22H32O4
- Molecular Weight:360.49
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Storage:Pure form -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Iloprost
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Histological Imaging/Staining
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IF
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WB
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RT-PCR
All Endogenous Metabolite Isoforms
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Biological Activity
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IP |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1 x 10-8 M
Compound: Iloprost
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Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells
Displacement of [3H]iloprost from human recombinant Prostanoid IP receptor expressed in HEK293 cells
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[PMID: 26988801] |
| HEK293 | IC50 |
1 x 10-8 M
Compound: Iloprost
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Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
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[PMID: 27876250] |
| HEK293 | IC50 |
1 x 10-2 μM
Compound: Iloprost
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Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
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[PMID: 27876250] |
Prostacyclin (PGI2) is synthesised in oviductal fluid and enhance the embryo development[1].
Iloprost is an PGI2 analog, and affects maturation and developmental competence of bovine oocytes[1].
Iloprost (0.5 μM; 22-24 h) increases blastocyst rates of bovine embryos as well as proportion of expanded blastocysts[1].
Iloprost (0.5 μM; 22-24 h) assists maturation rates and cumulus cell expansion of bovine oocytes, and increases the mRNA expression of genes related to cumulus expansion[1].
Iloprost (0.5 μM; 22-24 h) reduces the occurrence of apoptosis in COCs and promotes an anti-apoptotic balance in the transcription of genes involved in apoptosis (BAX and BCL2) [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Bovine oocytes: cumulus oocyte complexes (COCs)
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Concentration:0.5 μM
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Incubation Time:22-24 hours
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Result:Increased mRNA expression levels of cysteine proteinases cathepsins, including ADAM17, AREG, and TNFAIP6 23 and cathepsin genes (CTSK and CTSS).
Iloprost (0.2 mg/kg/d; i.p.; 10 d) attenuates hyperoxia effects and reduces inflammation in the newborn mouse lung, with Cyclooxygenase-2 (COX-2/PTGS2) mediates hyperoxia-induced impairment[3].
Iloprost (0.2 mg/kg; i.v. or i.p.) exhibits short half-life, and is often administered by means of frequent (every 2-4h) inhalation in treatment[4].
Comparison of pharmacokinetic parameter in rats and mice[4]
| Animal | Route | Dose (mg/kg) | AUC (ng•h/mL) | F (%) | CL (range) (mL/min/kg) | t1/2λi (min) | t1/2λz (min) |
| Mice | i.v. | 0.2 | 21.9 | 100 | 152 | 3 | 15 |
| Rat | i.g. | 0.2 | 2.2 | 10 | / | 4 | 58 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spontaneously metastasizing R 3327 MAT Lu prostate carcinoma in Cop rat[2]
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Dosage:0.3 mg/kg/min
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Administration:Subcutaneous administration via Alzet mini pumps; continuously for 33 days
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Result:Reduced the number of visible lung metastases, but had no effect on the growth of the primary tumor.
This action was based on the ability to reduce the attachment of tumor cells to platelets and to inhibit adhesion of tumor cells-platelet aggregates to the endothelial lining.
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Animal Model:Newborn C57BL/6 mice (4-day-old)[3]
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Dosage:0.2 mg/kg
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Administration:Intraperitoneal injection; once daily; 10 days
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Result:Reduced markedly pro-inflammatory cytokines IL-1β and TNF-α mRNA and protein.
Inhibited alveolar septation, reduced hyperoxia-induced total lung resistance and myeloperoxidase, prevented hyperoxia-reduced lung microvascular density.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 78919-13-8
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Appearance Oil
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Molecular Weight 360.49
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Formula C22H32O4
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Color Colorless to light yellow
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SMILES
O=C(O)CCC/C=C1C[C@@]2([H])C[C@@H](O)[C@H](/C=C/[C@@H](O)C(C)CC#CC)[C@@]2([H])C\1
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Synonyms
Ciloprost; ZK 36374
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
Prostaglandin I2 signaling prevents angiotensin II-induced atrial remodeling and vulnerability to atrial fibrillation in mice. [Abstract]2024 Jun 15;81(1):264. PMID: 38878214
Iloprost purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 Jun 15;81(1):264. [Abstract]
Representative Sirus red staining of left atrial tissues of Saline/Vehicle, Saline/Iloprost (0.2 mg/kg, i.p.), Ang II/Vehicle, and Ang II/Iloprost mice.
Iloprost purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 Jun 15;81(1):264. [Abstract]
Immunofluorescence staining of α-SMA (alpha-smooth muscle actin) and Vimentin. in left atrial tissues treated with Iloprost (0.2 mg/kg, i.p.).
Iloprost purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 Jun 15;81(1):264. [Abstract]
Western blot analysis of Collagen I, α-SMA and Periostin protein levels in the atrial tissues treated with Iloprost (0.2 mg/kg, i.p.).
Iloprost purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2024 Jun 15;81(1):264. [Abstract]
Mouse primary atrial fibroblasts were starved for 24 h and then treated with Ang II (1 µM) and/or iloprost (10 µM). Quantification of Col1a1 (collagen type I alpha 1 chain) and Acta2 (actin alpha 2) mRNA levels at 8 h.
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Cells
Blastocyst-Derived Lactic Acid May Regulate S100A6 Expression and Function in Mouse Decidualization via Stimulation of Uterine Epithelial Arachidonic Acid Secretion. [Abstract]2024 Jan 23;13(3):206. PMID: 38334598 -
Eur J Pharmacol
Cyclooxygenase-2 inhibition prevents renal toxicity but not hypertension during sunitinib treatment. [Abstract]2024 Jan 5:962:176199. PMID: 38029870 -
J Cell Mol Med
Iloprost Concentration-Dependently Attenuates Platelet Function and Apoptosis by Elevating PKA Activity. [Abstract]2025 Feb;29(3):e70403. PMID: 39929746 -
J Dent Sci
The additive effect of iloprost on the biological properties of Mineral trioxide aggregate on mesenchymal stem cells. [Abstract]2022 Jan;17(1):225-232. PMID: 35028042
Solvent & Solubility
DMSO : 100 mg/mL (277.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (420 KB)
- English - EN (420 KB)
- Français - FR (420 KB)
- Deutsch - DE (420 KB)
- Norwegian - NO (420 KB)
- Español - ES (420 KB)
- Swedish - SV (420 KB)
- Italian - IT (420 KB)
- Korean - KR (420 KB)
- Portuguese - PT (420 KB)
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Handling Instructions (2659 KB)
References
[1]. Kowalczyk-Zieba I, et al. Iloprost affects in vitro maturation and developmental competence of bovine oocytes. Theriogenology. 2020 Nov;157:286-296. [Content Brief]
[2]. Hildebrand M. Pharmacokinetics of iloprost and cicaprost in mice. Prostaglandins. 1992 Nov;44(5):431-42. [Content Brief]
[3]. Olave N, et al. Iloprost attenuates hyperoxia-mediated impairment of lung development in newborn mice. Am J Physiol Lung Cell Mol Physiol. 2018 Oct 1;315(4):L535-L544. [Content Brief]
[4]. Schneider MR, et al. Effects of prostacyclin analogues in in vivo tumor models. Adv Prostaglandin Thromboxane Leukot Res. 1991;21B:901-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7740 mL | 13.8700 mL | 27.7400 mL | 69.3501 mL |
| 5 mM | 0.5548 mL | 2.7740 mL | 5.5480 mL | 13.8700 mL | |
| 10 mM | 0.2774 mL | 1.3870 mL | 2.7740 mL | 6.9350 mL | |
| 15 mM | 0.1849 mL | 0.9247 mL | 1.8493 mL | 4.6233 mL | |
| 20 mM | 0.1387 mL | 0.6935 mL | 1.3870 mL | 3.4675 mL | |
| 25 mM | 0.1110 mL | 0.5548 mL | 1.1096 mL | 2.7740 mL | |
| 30 mM | 0.0925 mL | 0.4623 mL | 0.9247 mL | 2.3117 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6935 mL | 1.7338 mL | |
| 50 mM | 0.0555 mL | 0.2774 mL | 0.5548 mL | 1.3870 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4623 mL | 1.1558 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8669 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6935 mL |
- Iloprost
- 78919-13-8
- Ciloprost
- ZK 36374
- ZK36374
- ZK 36374
- ZK-36374
- Prostaglandin Receptor
- Endogenous Metabolite
- PGI2 analog
- in vitro maturation
- IVM
- embryo development
- anti-inflammation
- peripheral vascular diseases
- anti-metastatic
- tumor cell-platelet interaction
- in vitro fertilization
- Cyclooxygenase-2
- COX-2/PTGS2
- hyperoxia-induced impairment
- Inhibitor
- inhibitor
- inhibit