GLPBio

Iloprost

Catalog No.: GC15911Purity:>98.00%Synonyms: Ciloprost
Iloprost is a prostacyclin (PGI2) analog that affects platelet aggregation.

Products are for research use only. Not for human use. We do not sell to patients.


Iloprost
Cas No.: 78919-13-8
10mM (in 1mL DMSO)In Stock
$371.00
1
2mgIn Stock
$198.00
1
5mgIn Stock
$338.00
1

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Description

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

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.

Product Documents

Purity:>98.00%Appearance:An oil

Chemical Properties

CAS No.
78919-13-8
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
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
Molecular Formula
C22H32O4
Molecular Weight
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
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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