Iloprost (ZK 36374; Ciloprost) 是一种前列环素 PGI2 类似物，参与胚胎发育和炎症改善，抑制肿瘤转移。Iloprost 可用于外周血管疾病的研究。
| 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[1][2][3][4]. |
体外研究
(In Vitro) | Prostacyclin (PGI2) is synthesised in oviductal fluid and enhance the embryo development[1].
Iloprost is an PGI2 analog, and affects maturation and developmental competence of bovine oocytes[1].
Iloprost (0.5 μM; 22-24 h) increases blastocyst rates of bovine embryos as well as proportion of expanded blastocysts[1].
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[1].
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)[1].
RT-PCR[1] | Cell Line: | Bovine oocytes: cumulus oocyte complexes (COCs) | | Concentration: | 0.5 μM | | Incubation Time: | 22-24 hours | | Result: | Increased mRNA expression levels of cysteine proteinases cathepsins, including ADAM17, AREG, and TNFAIP6 23 and cathepsin genes (CTSK and CTSS). |
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体内研究
(In Vivo) | 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[2].
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[3].
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[4].
Comparison of pharmacokinetic parameter in rats and mice[4]
| Animal | Route | Dose (mg/kg) | AUC (ngoh/mL) | F (%) | CL (range) (mL/min/kg) | t1/2λi(min) | t1/2λz(min) | | Mice | i.v. | 0.2 | 21.9 | 100 | 152 | 3 | 15 | | Rat | i.g. | 0.2 | 2.2 | 10 | / | 4 | 58 |
| Animal Model: | Spontaneously metastasizing R 3327 MAT Lu prostate carcinoma in Cop rat[2] | | 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)[3] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Pure form | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(277.40 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7740 mL | 13.8700 mL | 27.7400 mL | | 5 mM | 0.5548 mL | 2.7740 mL | 5.5480 mL | | 10 mM | 0.2774 mL | 1.3870 mL | 2.7740 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 2.5 mg/mL (6.94 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.94 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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