Iloprost
(Synonyms: 伊洛前列素; Ciloprost; ZK 36374) 目录号 : GC15911
Iloprost是一种前列环素（PGI2）类似物，能够影响血小板聚集。
Cas No.:78919-13-8
Sample solution is provided at 25 µL, 10mM.
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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.
Iloprost是一种前列环素（PGI2）类似物，能够影响血小板聚集[1]。Iloprostzai在临床上用于治疗肺动脉高压（PAH）、硬皮病、雷诺现象、冻伤以及其他血管收缩导致血液无法流向组织的疾病[2, 3]。
在体外，Iloprost（200ng/mL）预处理肺内皮细胞15min，显著降低了脂多糖（LPS）诱导的FITC标记葡聚糖的透过率，减轻了脂多糖诱导的内皮细胞单层破坏[4]。Iloprost（1μM）处理人牙周膜细胞（hPDLs）24h，促进了细胞中VEGF 和COL1的mRNA和蛋白表达[5]。
在体内，Iloprost（1, 4 and 10μg/kg）通过口服治疗肠系膜动脉血栓形成模型小鼠，以剂量依赖性方式减轻了小鼠肠系膜小动脉中的血栓形成[6]。
| 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: | |
| Cas No. | 78919-13-8 | SDF | |
| 别名 | 伊洛前列素; Ciloprost; ZK 36374 | ||
| 化学名 | (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 | ||
| 分子式 | C22H32O4 | 分子量 | 360.49 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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