AS 101|106566-58-9|(AS101)-陌孚医药/Medlife

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AS 101 (Synonyms: AS101)

目录号: PC11588 纯度: ≥98%

CAS No. :106566-58-9

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中文名称	AS 101
中文别名	铵三氯[1,2-乙二醇-O,O']-碲酸盐;化合物AS101;AS 101,免疫调节剂
英文名称	AS 101
英文别名	Tellurate(1-),trichloro[1,2-ethanediolato(2-)-kO1,kO2]-, ammonium (1:1), (SP-5-22)-;AMMONIUM TRICHLORO[1,2-ETHANEDIOLATO-O,O']-TELLURATE;AS 101;A16414;CID 9839786;1,3,2-Dioxatellurolane, 2,2,2-trichloro-2,2,2,2-tetrahydro-, ammoniate (1:1);Ammonium trichlorotellurate;AS101;Ammonium trichloro(dioxoethylene-O,O')tellurate;AS-101 (pharmaceutical);Ossirene;Tellurate(1-), (1,2-ethanediolato(2-)-O,O')trichloro-, ammonium, (SP-5-22)-
Cas No.	106566-58-9
分子式	C₂H₈Cl₃NO₂Te
分子量	312.05
包装储存	-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.

性状

Solid

IC50 & Target[1][2]

IL-1β

IL-10

Caspase-1

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.
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.
Ossirene (0.1, 0.5, 1, 2.5 μg/mL) significantly decreases B16 melanoma, stomach adenocarcinoma, and human glioblastoma multiforme (GBM) cells proliferation.
AS101 (0.5 μg/mL; for 24 hours) sensitizes GBM tumor cells to paclitaxel in an IL-10-dependent manner.

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

Western Blot Analysis

Cell Line:	B16 melanoma cells
Concentration:	1 μg/mL
Incubation Time:	For 24 hours
Result:	Almost completely abrogated expression of pStat3.

RT-PCR

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.

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.

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

Animal Model:	SCID mice with GBM cells
Dosage:	0.5 mg/kg
Administration:	IP; daily; 25 days
Result:	Significantly increased survival of GBM tumor-bearing mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

ClinicalTrial

参考文献

[1]. Diamond Ling, et al. The Tellurium Redox Immunomodulating Compound AS101 Inhibits IL-1β-activated Inflammation in the Human Retinal Pigment Epithelium. Br J Ophthalmol. 2013 Jul;97(7):934-8. [Information]

[2]. Sredni B, et al. Ammonium trichloro(dioxoethylene-o,o)tellurate (AS101) sensitizes tumors to chemotherapy by inhibiting the tumor interleukin 10 autocrine loop. Cancer Res. 2004 Mar 1;64(5):1843-52. [Information]

[3]. Yona Kalechman, et al. Inhibition of interleukin-10 by the Immunomodulator AS101 Reduces Mesangial Cell Proliferation in Experimental Mesangioproliferative Glomerulonephritis: Association With Dephosphorylation of STAT3. J Biol Chem. 2004 Jun 4;279(23):24 [Information]

[4]. Yafit Hachmo, et al. The Small Tellurium Compound AS101 Ameliorates Rat Crescentic Glomerulonephritis: Association With Inhibition of Macrophage Caspase-1 Activity via Very Late Antigen-4 Inactivation. Front Immunol. 2017 Mar 7;8:240. [Information]

溶解度数据

体外研究:

DMSO : 12.5 mg/mL (40.06 mM; ultrasonic and warming and heat to 80°C)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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 (stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 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.

建议依照次序添加每种溶剂： 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。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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