Ossirene (AS101) 是一种免疫调节性碲化合物,有效的IL-1β抑制剂。Ossirene 通过抑制IL-10消除 STAT3 的磷酸化。Ossirene 有效抑制Caspase-1,可用于自身免疫性疾病和某些恶性肿瘤。
生物活性 | Ossirene (AS101), an immunomodulatory tellurium compound, is a potentIL-1βinhibitor[1]. Ossirene abolishes phosphorylation ofSTAT3by inhibitingIL-10. Ossirene potently inhibitsCaspase-1and is used for the autoimmune diseases and certain malignancies[2][3][4]. |
IC50& Target[1][2][4] | |
体外研究 (In Vitro) | Ossirene (AS101; 1 μg/mL; for 24 hours) almost completely abrogates expression of pStat3. Ossirene may reduce expression of Bcl-2 after inhibition of Stat3 activation via IL-10 inhibition[2]. AS101 (0.5, 5 mg/mL; 24 hours) inhibits IL-1β-induced mRNA expression of inflammatory mediators in the RPE in a dose-dependent manner. AS101 inhibits IL-1β-induced mRNA expression and protein production of IL-6 and IL-8 in RPE cells. AS101 (5 mg/mL; 1 hour) inhibits the phosphorylation of the p65 component of the NFκB complex activated by IL-1β[1]. Ossirene (0.1, 0.5, 1, 2.5 μg/mL) significantly decreases B16 melanoma, stomach adenocarcinoma, and human glioblastoma multiforme (GBM) cells proliferation[2]. AS101 (0.5 μg/mL; for 24 hours) sensitizes GBM tumor cells to paclitaxel in an IL-10-dependent manner[2].
Western Blot Analysis[2] Cell Line: | B16 melanoma cells | Concentration: | 1 μg/mL | Incubation Time: | For 24 hours | Result: | Almost completely abrogated expression of pStat3. |
RT-PCR[1] Cell Line: | ARPE19 cells | Concentration: | 0.5, 5 mg/mL | Incubation Time: | 24 hours | Result: | Inhibited IL-1β-induced mRNA expression of inflammatory mediators in the RPE in a dose-dependent manner. |
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体内研究 (In Vivo) | Ossirene (AS101; 0.5 mg/kg/day; IP; 25 days) sensitizes GBM tumors to paclitaxel via inhibition of IL-10, resulting in increased survival[2].
Animal Model: | SCID mice with GBM cells[2] | Dosage: | 0.5 mg/kg | Administration: | IP; daily; 25 days | Result: | Significantly increased survival of GBM tumor-bearing mice. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
溶解性数据 | In Vitro: DMSO : 12.5 mg/mL(40.06 mM;ultrasonic and warming and heat to 80℃) 配制储备液 1 mM | 3.2046 mL | 16.0231 mL | 32.0461 mL | 5 mM | 0.6409 mL | 3.2046 mL | 6.4092 mL | 10 mM | 0.3205 mL | 1.6023 mL | 3.2046 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 (stored under nitrogen)。-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: 1.25 mg/mL (4.01 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (4.01 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 12.5 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: 1.25 mg/mL (4.01 mM); Suspended solution; Need ultrasonic
此方案可获得 1.25 mg/mL (4.01 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (4.01 mM); Clear solution
此方案可获得 ≥ 1.25 mg/mL (4.01 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 12.5 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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