生物活性分子抑制剂Piclidenoson(Synonyms: IB-MECA; CF-101)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
Piclidenoson (Synonyms: IB-MECA; CF-101) 纯度: 99.32%

Piclidenoson (IB-MECA) 是一种首创的,具有口服活性的,选择性的腺苷 A3 受体 (A3AR) 激动剂。Piclidenoson 在不同类型的癌细胞如黑色素瘤、白血病中表现出抗增殖和诱导凋亡 (apoptosis) 的作用。Piclidenoson 可用于自身免疫性炎症疾病和 COVID-19 的研究。

Piclidenoson(Synonyms: IB-MECA;  CF-101)

Piclidenoson Chemical Structure

CAS No. : 152918-18-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1459 In-stock
2 mg ¥800 In-stock
5 mg ¥1300 In-stock
10 mg ¥2200 In-stock
25 mg ¥4400 In-stock
50 mg ¥7400 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Piclidenoson 相关产品

相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Small Molecule Immuno-Oncology Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • Neurotransmitter Receptor Compound Library
  • Anti-Blood Cancer Compound Library
  • Rare Diseases Drug Library

生物活性

Piclidenoson (IB-MECA) is a first-in-class, orally active and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19[1][2][3][4].

IC50 & Target

A3AR[2]

体外研究
(In Vitro)

Piclidenoson is able to inhibit Forskolin (HY-15371)-stimulated cAMP levels with EC50s of 0.82 μM and 1.2 μM in OVCAR-3 cells and Caov-4 cells, respectively[2].
Piclidenoson (0.0001-100 μM; 48 hours) significantly reduces cell viability in a dose-dependent manner in human ovarian cancer cell lines, with IC50s of 32.14 μM and 45.37 μM for OVCAR-3 and Caov-4 cells, respectively[2].
Piclidenoson (0.001-100 μM; 48 hours) induces apoptosis in ovarian cancer cell line through the caspase pathway[2].
Piclidenoson induces apoptosis via the mitochondrial signaling pathway[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 0.0001-100 μM
Incubation Time: 48 hours
Result: Resulted in a dose-dependent reduction in the cell viability.

Apoptosis Analysis[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 0.1 μM, 1 μM, 10 μM, 50 μM, 100 μM
Incubation Time: 48 hours
Result: Significant increased in the percentage of apoptosis in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: OVCAR-3 cells, Caov-4 cells
Concentration: 1 μM, 10 μM, 100 μM
Incubation Time: 48 hours
Result: Decreased the expression of Bcl-2 was noticeably and increased the expression of Bax protein.

体内研究
(In Vivo)

Piclidenoson (105 μg/kg; i.p.) enhances survival of γ-irradiated mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B10CBAF1 male mice aged 3 months (average 30 g)[1]
Dosage: 105 μg/kg
Administration: Intraperitoneal injection, 0.5 h after irradiation
Result: Resulted in statistically significant increases of the mean survival time in comparison with the control irradiated mice.

Clinical Trial

分子量

510.29

Formula

C18H19IN6O4

CAS 号

152918-18-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 45 mg/mL (88.19 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9597 mL 9.7983 mL 19.5967 mL
5 mM 0.3919 mL 1.9597 mL 3.9193 mL
10 mM 0.1960 mL 0.9798 mL 1.9597 mL

*

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, 6 months; -20°C, 1 month。-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。

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
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

  • 1.

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.90 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Shin Y, et al. Activation of Phosphoinositide Breakdown and Elevation of Intracellular Calcium in a Rat RBL-2H3 Mast Cell Line by Adenosine Analogs: Involvement of A(3)-Adenosine Receptors? Drug Dev Res. 1996 Sep 1;39(1):36-46.

    [2]. Abedi H, et al. Mitochondrial and caspase pathways are involved in the induction of apoptosis by IB-MECA in ovarian cancer cell lines. Tumour Biol. 2014 Nov;35(11):11027-11039.

    [3]. Hofer M, et al. Agonist of the adenosine A3 receptor, IB-MECA, and inhibitor of cyclooxygenase-2, meloxicam, given alone or in a combination early after total body irradiation enhance survival of γ-irradiated mice. Radiat Environ Biophys. 2014 Mar;53(1):211-215.

    [4]. Chandan Sarkar, et al. Potential Therapeutic Options for COVID-19: Current Status, Challenges, and Future Perspectives. Front Pharmacol. 2020; 11: 572870.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务