1. GPCR/G Protein Metabolic Enzyme/Protease
  2. Prostaglandin Receptor Endogenous Metabolite
  3. Iloprost

Iloprost  (Synonyms: 伊洛前列素; Ciloprost; ZK 36374)

目录号: HY-A0096 纯度: 99.76%
COA 产品使用指南

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。

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Iloprost Chemical Structure

Iloprost Chemical Structure

CAS No. : 78919-13-8

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10 mM * 1 mL in DMSO ¥5720
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2 mg ¥2350
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5 mg ¥5200
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Other Forms of Iloprost:

查看 Prostaglandin Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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].

IC50 & Target

IP

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Cell line IC50
2.5 nM
Compound: Iloprost
Inhibition concentration against ADP-induced platelet aggregation using human platelet rich plasma
Inhibition concentration against ADP-induced platelet aggregation using human platelet rich plasma
[PMID: 15914004]
HEK293 IC50
1 x 10-2 μM
Compound: Iloprost
Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
Displacement of [3H]iloprost from human recombinant IP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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).
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 (ng•h/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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
分子量

360.49

Formula

C22H32O4

CAS 号
性状

油状物

颜色

Colorless to light yellow

中文名称

伊洛前列素;亚罗普斯特

结构分类
初始来源
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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (277.40 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7740 mL 13.8700 mL 27.7400 mL
5 mM 0.5548 mL 2.7740 mL 5.5480 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

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分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.94 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.94 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.76%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7740 mL 13.8700 mL 27.7400 mL 69.3501 mL
5 mM 0.5548 mL 2.7740 mL 5.5480 mL 13.8700 mL
10 mM 0.2774 mL 1.3870 mL 2.7740 mL 6.9350 mL
15 mM 0.1849 mL 0.9247 mL 1.8493 mL 4.6233 mL
20 mM 0.1387 mL 0.6935 mL 1.3870 mL 3.4675 mL
25 mM 0.1110 mL 0.5548 mL 1.1096 mL 2.7740 mL
30 mM 0.0925 mL 0.4623 mL 0.9247 mL 2.3117 mL
40 mM 0.0694 mL 0.3468 mL 0.6935 mL 1.7338 mL
50 mM 0.0555 mL 0.2774 mL 0.5548 mL 1.3870 mL
60 mM 0.0462 mL 0.2312 mL 0.4623 mL 1.1558 mL
80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8669 mL
100 mM 0.0277 mL 0.1387 mL 0.2774 mL 0.6935 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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