Iloprost

目录号: GC15911纯度: >98.00%同义词: 伊洛前列素; Ciloprost; ZK 36374
Iloprost是一种前列环素(PGI2)类似物,能够影响血小板聚集。

Iloprost
Cas No.: 78919-13-8
规格价格库存数量操作
2mg¥1,980.00现货
1
5mg¥3,375.00现货
1
10mM (in 1mL DMSO)¥3,713.00现货
1

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产品描述 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.

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]

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
78919-13-8
同义词
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
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 g/mol
溶解性
DMF: 30 mg/ml,DMSO: 25 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 1 mg/ml
保存条件
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°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

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