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编 号:F460000
分子式:C22H32O4
分子量:360.49
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10mM*1mL in DMSO
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2mg
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5mg
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10mg
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生物活性:
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.

体内研究:
Iloprost (0.3 mg/kg/min; via s.c. mini pumps; 33 d) has a significant anti-metastatic activity in a spontaneously metastasizing tumor model in rat.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.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.Comparison of pharmacokinetic parameter in rats and miceAnimalRouteDose (mg/kg)AUC (ng?h/mL)F (%)CL (range) (mL/min/kg)t1/2λi (min)t1/2λz (min)
Micei.v.0.221.9100152315
Rati.g.0.22.210/458
Animal Model:Spontaneously metastasizing R 3327 MAT Lu prostate carcinoma in Cop rat
Dosage:0.3 mg/kg/min
Administration:Subcutaneous administration via Alzet mini pumps; continuously for 33 days
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.
Animal Model:Newborn C57BL/6 mice (4-day-old)
Dosage:0.2 mg/kg
Administration:Intraperitoneal injection; once daily; 10 days
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.

体外研究:
Prostacyclin (PGI2) is synthesised in oviductal fluid and enhance the embryo development.Iloprost is an PGI2 analog, and affects maturation and developmental competence of bovine oocytes. Iloprost (0.5 μM; 22-24 h) increases blastocyst rates of bovine embryos as well as proportion of expanded blastocysts.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.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) .
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