D609 是一种抗肿瘤黄原酸盐，一种特异性、竞争性的磷脂酰胆碱特异性磷脂酶 C (PC-PLC) 抑制剂，Ki为 6.4 μM。D609 是一种抗氧化保护剂，也具有抗病毒和抗炎活性。
| 生物活性 | D609, an antitumoural xanthate, is a specific and competitivephosphatidyl choline-specificphospholipaseC (PC-PLC)inhibitor with aKiof 6.4 μM. D609 is an antioxidative protector and has antiviral and anti-inflammatory activity[1][2][3]. |
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体外研究
(In Vitro) | D609 (100 μM; for 2 h) significantly attenuats the proliferation of various cell lines[2].
D609 (50, 100 and 200 μM; for 2 h) results in caspase-3 activation with 200 μM and causes no detectable cleavage with 50, 100 μM[2].
D609 (100 μM; for 2 h) significantly inhibits BrdU incorporation in BV-2 microglia and causes accumulation of cells in G1 phase with decreased number of cells in the S phase[2].
D609 (100 μM; for 2 h and cultured for an additional 2 h or 22 h without D609) increases ceramide levels, up-regulates p21 expression and causes a decreases in phospho-Rb[2].
Cell Proliferation Assay[2] | Cell Line: | RAW 264.7 macrophages, N9 and BV-2 microglia, and DITNC1 astrocytes | | Concentration: | 100 μM | | Incubation Time: | For 2 hours | | Result: | Significantly attenuated the proliferation of RAW 264.7 macrophages, N9 and BV-2 microglia, and DITNC1 astrocytes, without affecting cell viability. |
Apoptosis Analysis[2] | Cell Line: | BV-2 cells | | Concentration: | 50, 100 and 200 μM | | Incubation Time: | For 2 hours | | Result: | Activated caspase-3 in a dose- and time-dependent manner. |
Cell Cycle Analysis[2] | Cell Line: | BV-2 cells | | Concentration: | 100 μM | | Incubation Time: | For 2 hours | | Result: | Significantly inhibited BrdU incorporation in BV-2 microglia and caused accumulation of cells in G1 phase with decreased number of cells in the S phase. |
Western Blot Analysis[2] | Cell Line: | BV-2 cells | | Concentration: | 100 μM | | Incubation Time: | For 2 hours | | Result: | Increased ceramide levels, up-regulated p21 expression and causes a decreased in phospho-Rb. |
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体内研究
(In Vivo) | D609 (2.5, 10 mg/kg/day; ip; for 6 weeks) inhibits the progression of preexisting atherosclerotic lesions in apoE-/-mice and changes the lesion composition into a more stable phenotype[3].
D609 (50 mg/kg; ip; single dose) for 30 min before intratracheal administration of LPS (3 mg/kg) prevents the development of LPS-induced pulmonary hypertension in adult male Wistar rats[4].
| Animal Model: | 26-week-old apoE–/–and C57BL/6 WT mice[3] | | Dosage: | 2.5, 10 mg/kg | | Administration: | IP; per day for 6 weeks | | Result: | Inhibited the progression of preexisting atherosclerotic lesions in apoE–/–mice and changed the lesion composition into a more stable phenotype.
Significantly decreased the aortic endothelial expression of the vascular cell adhesion molecule-1 and the intercellular adhesion molecule-1. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(375.29 mM;Need ultrasonic) H2O : 2 mg/mL(7.51 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.7529 mL | 18.7645 mL | 37.5291 mL | | 5 mM | 0.7506 mL | 3.7529 mL | 7.5058 mL | | 10 mM | 0.3753 mL | 1.8765 mL | 3.7529 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： PBS Solubility: 25 mg/mL (93.82 mM); Clear solution; Need ultrasonic and warming and heat to 60℃ 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 3 mg/mL (11.26 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (11.26 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 30.0 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 3 mg/mL (11.26 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (11.26 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 30.0 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。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 3 mg/mL (11.26 mM); Clear solution
此方案可获得 ≥ 3 mg/mL (11.26 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 30.0 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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