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Iloprost (Synonyms: Ciloprost)

Catalog No.GC15911 Copy One-Click Copy Product Info

Iloprost is a prostacyclin (PGI2) analog that affects platelet aggregation.

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Iloprost Chemical Structure

Cas No.: 78919-13-8

Size Price Stock Qty
10mM (in 1mL DMSO)
$371.00
In stock
2mg
$198.00
In stock
5mg
$338.00
In stock

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Sample solution is provided at 25 µL, 10mM.



Description of Iloprost

Iloprost is a prostacyclin (PGI2) analog that affects platelet aggregation[1]. Clinically, Iloprost is used to treat pulmonary arterial hypertension (PAH), scleroderma, Raynaud's phenomenon, frostbite, and other conditions characterized by impaired blood flow to tissues due to vasoconstriction[2, 3].

In vitro, pretreatment of pulmonary endothelial cells with Iloprost (200ng/mL) for 15min significantly reduced the permeability of FITC-labeled dextran induced by lipopolysaccharide (LPS), mitigating LPS-induced disruption of the endothelial cell monolayer[4]. Treatment of human periodontal ligament cells (hPDLs) with Iloprost (1μM) for 24h promoted the mRNA and protein expression of VEGF and COL1 in the cells[5].

In vivo, oral administration of Iloprost (1, 4, and 10μg/kg) to mice in a mesenteric artery thrombosis model reduced thrombosis in the mesenteric arterioles in a dose-dependent manner[6].

 References:
[1] Kobzar G, Mardla V, Järving I, et al. Comparison of anti-aggregatory effects of PGI2, PGI3 and iloprost on human and rabbit platelets[J]. Cellular Physiology and Biochemistry, 2001, 11(5): 279-284.
[2] Foti R. Treatment with intravenous iloprost in patients with systemic sclerosis: A short review[J]. Journal of Rare Diseases Research & Treatment, 2017, 2(4).
[3] Ruiz J, Watford M, Samuel E, et al. Corticotrophins, corticosteroids, and prostaglandins[M]//Side Effects of Drugs Annual. Elsevier, 2020, 42: 407-415.
[4] Birukova A A, Wu T, Tian Y, et al. Iloprost improves endothelial barrier function in lipopolysaccharide-induced lung injury[J]. European Respiratory Journal, 2012, 41(1): 165-176.
[5] Jearanaiphaisarn T, Sanharati T, Pavasant P, et al. The effect of iloprost on cell proliferation and angiogenesis-related gene expression in human periodontal ligament cells[J]. Odontology, 2018, 106(1): 11-18.
[6] Wang X, Chen S, Wan J, et al. Iloprost Concentration‐Dependently Attenuates Platelet Function and Apoptosis by Elevating PKA Activity[J]. Journal of Cellular and Molecular Medicine, 2025, 29(3): e70403.

Protocol of Iloprost

Cell experiment [1]:

Cell lines

Pulmonary endothelial cells

Preparation Method

Pulmonary endothelial cells were pre-incubated with Iloprost (200ng/mL) or Br-cAMP (500ng/mL) for 15min followed by an LPS (300ng/mL) 5-h challenge and measurements of permeability for fluorescein isothiocyanate (FITC)-labelled dextran. Permeability data are presented as the mean±sd of 8 independent experiments.

Reaction Conditions

200ng/mL; 15min

Applications

Both Iloprost and Br-cAMP attenuated LPS-induced permeability for FITC-labelled dextran.

Animal experiment [2]:

Animal models

C57BL/6J WT mice

Preparation Method

After oral administration of different doses of Iloprost (1, 4 and 10μg/kg) in mice for 20 min, the recipient mice were anaesthetised with 2% pentobarbital (100mg/kg, i.p.). Mice were injected i.v. with calcein-labelled platelets (5×106/g) of matching genotype. The mesentery vascular bed was exteriorised, and one arteriole was chosen and visualised and recorded with an inverted fluorescent microscope. Thrombus formation was induced by topical application of a 1-mm2 filter paper soaked with 6% FeCl3. The vessel occlusion time was defined as the time to complete cessation of blood flow.

Dosage form

1, 4 and 10μg/kg; p.o.

Applications

As the doses of oral administration of Iloprost increased, mice exhibited delayed and diminished thrombus formation, and mean occlusion time became significantly longer in the mice compared with vehicle control, and in all observed groups, 10μg/kg Iloprost exhibited the strongest antithrombotic effect.

References:
[1] Birukova A A, Wu T, Tian Y, et al. Iloprost improves endothelial barrier function in lipopolysaccharide-induced lung injury[J]. European Respiratory Journal, 2012, 41(1): 165-176.
[2]Wang X, Chen S, Wan J, et al. Iloprost Concentration?Dependently Attenuates Platelet Function and Apoptosis by Elevating PKA Activity[J]. Journal of Cellular and Molecular Medicine, 2025, 29(3): e70403.

Chemical Properties of Iloprost

Cas No. 78919-13-8 SDF
Synonyms Ciloprost
Chemical Name (E)-5-((3aS,4R,5R,6aS)-5-hydroxy-4-((3S,4R,E)-3-hydroxy-4-methyloct-1-en-6-yn-1-yl)hexahydropentalen-2(1H)-ylidene)pentanoic acid
Canonical SMILES O[C@H]1[C@H](/C=C/[C@H]([C@H](C)CC#CC)O)[C@@H](C/C2=C/CCCC(O)=O)[C@@H](C2)C1
Formula C22H32O4 M.Wt 360.49
Solubility DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 1 mg/ml Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Iloprost

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.774 mL 13.87 mL 27.74 mL
5 mM 554.8 μL 2.774 mL 5.548 mL
10 mM 277.4 μL 1.387 mL 2.774 mL
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In vivo Formulation Calculator (Clear solution) of Iloprost

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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