铵三氯[1,2-乙二醇-O,O']-碲酸盐

铵三氯[1,2-乙二醇-O,O']-碲酸盐用途

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。

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铵三氯[1,2-乙二醇-O,O']-碲酸盐名称

[ CAS 号 ]:
106566-58-9

[ 中文名 ]:
铵三氯[1,2-乙二醇-O,O']-碲酸盐

[ 英文名 ]:
AS 101

[英文别名 ]:

AS 101

铵三氯[1,2-乙二醇-O,O']-碲酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 免疫及炎症 >> 白细胞介素相关

信号通路 >> 细胞凋亡 >> 胱天蛋白酶

研究领域 >> 炎症/免疫

[ 靶点 ]

IL-1β

IL-10

Caspase-1

[体外研究]

骨化(AS101；1μg/mL；24小时)几乎完全抑制pStat3的表达。通过IL-10抑制Stat3激活后,骨化可能降低Bcl-2的表达[2]。AS101(0.5,5mg/mL；24小时)以剂量依赖性方式抑制IL-1β诱导的RPE炎症介质mRNA表达。AS101抑制IL-1β诱导的RPE细胞IL-6和IL-8的mRNA表达和蛋白生成。AS101(5mg/mL；1h)抑制IL-1β激活的NF-κB复合物p65组分的磷酸化[1]。骨化(0.1,0.5,1,2.5μg/mL)可显著抑制B16黑色素瘤、胃腺癌和人多形性胶质母细胞瘤(GBM)细胞增殖[2]。AS101(0.5μg/mL；24小时)以IL-10依赖的方式使GBM肿瘤细胞对紫杉醇敏感[2]。Western Blot分析[2]细胞株：B16黑色素瘤细胞浓度：1μg/mL孵育时间：24小时结果：pStat3表达几乎完全消失。RT-PCR[1]细胞株：ARPE19细胞浓度：0.5,5mg/mL孵育时间：24小时结果：抑制IL-1β诱导的RPE炎症介质mRNA表达,呈剂量依赖性。

[体内研究]

骨化(AS101；0.5 mg/kg/天；IP；25天)通过抑制IL-10使GBM肿瘤对紫杉醇敏感,从而提高生存率[2]。动物模型：具有GBM细胞的SCID小鼠[2]剂量：0.5mg/kg给药：IP；每日；25天结果：GBM荷瘤小鼠生存率显著提高。

[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.

[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.

[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):24724-32.

[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.

铵三氯[1,2-乙二醇-O,O']-碲酸盐物理化学性质

[ 密度 ]:
1.097g/cm3

[ 沸点 ]:
197.5ºC at 760mmHg

[ 分子式 ]:
C₂H₈Cl₃NO₂Te

[ 分子量 ]:
312.04900

[ 闪点 ]:
108.2ºC

[ 精确质量 ]:
312.86800

[ PSA ]:
18.46000

[ LogP ]:
2.01210

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

[ 水溶解性 ]:
Soluble to 5 mM in DMSO and to 5 mM in ethanol

铵三氯[1,2-乙二醇-O,O']-碲酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WY2310000

CHEMICAL NAME :: Tellurate(1-), (1,2-ethanediolato(2-)-O,O')trichloro-, ammonium, (SP-5-22)-

CAS REGISTRY NUMBER :: 106566-58-9

LAST UPDATED :: 199707

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C2-H4-Cl3-O2-Te.H4-N

MOLECULAR WEIGHT :: 312.06

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

REFERENCE :: NICRDR Natural Immunity and Cell Growth Regulation. (S. Karger Publishers, Inc., 79 Fifth Ave., New York, NY 10003 USA) V.3- 1984- Volume(issue)/page/year: 7,163,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

REFERENCE :: NICRDR Natural Immunity and Cell Growth Regulation. (S. Karger Publishers, Inc., 79 Fifth Ave., New York, NY 10003 USA) V.3- 1984- Volume(issue)/page/year: 7,163,1988 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 96 mg/kg/4W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - retinal changes (pigmentary depositions, retinitis, other)

REFERENCE :: TOPADD Toxicologic Pathology. (c/o Dr. F.A. de la Iglesia, Warner-Lambert Co., Pharmaceutical Research Div., POB 1047, Ann Arbor, MI 48106) V.6(3/4)- 1978- Volume(issue)/page/year: 17,799,1989