Rosiglitazone 罗格列酮


描述

Rosiglitazone 罗格列酮

 

产品标签

Rosiglitazone罗格列酮;BRL 49653;PPARγ激动剂;降血糖药物;胰岛素曾敏剂;CAS:122320-73-4;

产品信息: 

产品名称

产品编号 CAS NO. 规格 价格(元)

Rosiglitazone罗格列酮

MZ9001-50MG 19545-26-7 50mg 300

Rosiglitazone罗格列酮

MZ9001-100MG 19545-26-7 100mg 450
Rosiglitazone罗格列酮 MZ9001-250MG 19545-26-7 250mg

850

Rosiglitazone罗格列酮 MZ9001-500MG 19545-26-7 500mg

1260

Rosiglitazone罗格列酮 MZ9001-1G 19545-26-7 1g

1980

产品描述

罗格列酮(Rosiglitazone)是一种有效且选择性的PPARγ激动剂,结合于PPARγ的配体结合域(LBD)结合,Kd值为43nM[1]。以细胞为基础的报告基因实验中发现,罗格列酮(10mM)选择性活化含PPARγLBD的嵌合体,对PPARα和PPARδ几乎无反应。在报告基因实验中,罗格列酮还激活全长序列的PPARγ1和PPARγ2,EC50分别是30nM和100nM。

罗格列酮(1 μM)能诱导C3H10T1/2干细胞分化为脂肪细胞。通过高脂高糖饲料结合链脲佐菌素(STZ)建立的大鼠II型糖尿病模型中,罗格列酮(4mg/kg)能够降低糖化血红蛋白(HbA1c)和空腹血糖水平[2]。控制性皮层撞击引起的创伤性脑损伤模型(TBI)中,罗格列酮(6mg/kg)降低小鼠大脑皮层中的挫伤体积、巨噬细胞浸润和小胶质细胞激活,以及抑制IL-6、MCP1、ICAM1、Caspase-3和Bax的表达,具有神经保护作用[3]。罗格列酮(ACSL4抑制剂)用于糖尿病肾病(DN)模型中,能提高存活率和改善肾脏功能,降低脂质过氧化产物MDA和铁离子的表达[4]。

产品特性

化学名:5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione
同义名:BRL 49653;罗格列酮碱; CAS NO:122320-73-4
分子式:C18H19N3O3S 分子量:357.43
纯度:≥99% 外观:白色或类白色结晶性粉末
溶解性:溶于DMSO (70mg/ml)、DMF(~25mg/ml);溶于甲醇;几乎不溶于乙醇和水;
化学结构式:

保存与运输方法

保存:2-8ºC密封干燥保存,至少2年有效。

运输:室温运输。

注意事项

1) 本品仅用作科研用途,不得用作临床诊断或治疗,不得用于食品或药品,绝对禁止用在人身上。

2) 为了您的安全和健康,请穿实验服并戴一次性手套操作。

参考文献

[1] Lehmann, J.M., et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ). J. Biol. Chem. 270(22), 12953-12956 (1995).

[2] Zhou, J.Y., et al. Chronic effects of berberine on blood, liver glucolipid metabolism and liver PPARs expression in diabetic hyperlipidemic rats. Biological and Pharmaceutical Bullentin 31(6), 1169-1176 (2008).

[3] Yi, J.-H.,et al. PPARγ agonist rosiglitazone is neuroprotective after traumatic brain injury via anti-inflammatory and anti-oxidative mechanisms. Brain Res. 1244, 164-172 (2008).

[4] Wang Y. et al. Ferroptosis involves in renal tubular cell death in diabetic nephropathy. European Journal of Pharmacology Volume 888, 5 December 2020, 173574.

储存液制备

          质量

溶剂体积

浓度

1mg 5mg 10mg
1mM 2.7978 mL 13.9888 mL 27.9775 mL
5mM 0.5596 mL 2.7978 mL 5.5955 mL
10mM 0.2798 mL 1.3989 mL 2.7978 mL

使用方法【源自文献,仅作参考】

文献1,Huang G.d.,et al.Synergy between peroxisome proliferator‐activated receptorγagonist and radiotherapy in cancer. Cancer Sci. 2018 Jul;109(7):2243-2255. PMID: 29791764

体内研究:

动物模型(Animal Model):CT26 and 4T1 xenograft models (female BALB/c mouse)

实验方法(Assay):When the tumor size reached approximately 50-100 mm3 or 200-300 mm3, the mice were randomly divided into 4-6 groups for CT26 (n = 6 for each group) and 4T1 models (n = 6 for each group). To investigate the therapeutic effect of rosiglitazone combined with RT, the mice were given 100 mg/kg rosiglitazone or vehicle (DMSO: PEG300: Tween80: ddH2O = 4:30:5:100) by oral gavage per day for 2 weeks. Before 6 or 12 Gy irradiation, each mouse was anesthetized and shielded by a lead box with only the tumor exposed.

给药途径(Administration):Oral gavage

文献2,Yi, J.-H.,et al. PPARγ agonist rosiglitazone is neuroprotective after traumatic brain injury via anti-inflammatory and anti-oxidative mechanisms. Brain Res. 1244, 164-172 (2008). PMID: 18948087

体内研究:

动物模型(Animal Model):TBI model of adult male C57BL/6 mice

实验方法(Assay):To cohorts of mice, rosiglitazone (6 mg/kg) or GW9662 (4 mg/kg; PPARγ antagonist) or vehicle (4% DMSO) was injected i.p. at 5 min, 6 h and 24 h after TBI.

给药途径(Administration):Intraperitoneal (i.p.) injection

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