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。
| 生物活性 | Piclidenoson (IB-MECA) is a first-in-class, orally active and selectiveA3adenosine receptor(A3AR)agonist. Piclidenoson exhibits antiproliferative effect and inducesapoptosisin differentcancercell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19[1][2][3][4]. |
| IC50& Target | |
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].
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].
| 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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 | 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℃, 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
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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 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 (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本网站选购。
|
m.cnreagent.com