Rosiglitazone.|122320-73-4|(罗格列酮; BRL 49653)-陌孚医药/Medlife

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Rosiglitazone. (Synonyms: 罗格列酮; BRL 49653)

目录号: PC12474 纯度: ≥98%

CAS No. :122320-73-4

商品编号	规格	价格	会员价
PC12474-25mg	25mg	¥490.00	请登录
PC12474-100mg	100mg	¥686.00	请登录
PC12474-200mg	200mg	¥1078.00	请登录
PC12474-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称

Rosiglitazone.

中文别名

罗格列酮;文迪雅;罗格利酮;罗格利酮碱;罗格列酮盐酸;罗格列酮盐酸盐;5-(4-(2-(甲基(吡啶-2-基)氨基)乙氧基)苄基)四氢噻唑-2,4-二酮;5-[[4-[2-(甲基-2-吡啶基氨基)乙氧基]苯基]甲基-2,4.噻唑烷二酮;5-[[4-[2-(甲基-2-吡啶氨基)乙氧基]苯基]甲基]-2,4-噻唑烷二酮;5-{4-[2-(N-甲基-2-吡啶基)氨基]乙氧基}苄基}-2,4-噻唑烷二酮;5-甲砜基吡啶-2-甲酸甲酯;N-[(1R)-2-氨基-1-甲基乙基]氨基甲酸叔丁酯;兰索拉唑;罗格列酮-D4;罗格列酮标准品;罗格列酮碱;马来酸罗格列酮;偏铌(Ⅴ)酸钙;盐酸罗格列酮;罗西格列酮;酒石酸罗格列酮;罗格列酮钠;瑞格列酮;罗格列酮碱(标准品);罗格列酮/罗格列酮碱;50MG/1G/1KG

英文名称

Rosiglitazone

英文别名

5-(4-(2-(Methyl(pyridin-2-yl)amino)ethoxy)benzyl)thiazolidine-2,4-dione;5-(4-[2-(METHYL-PYRIDIN-2-YL-AMINO)-ETHOXY]-BENZYL)-THIAZOLIDINE-2,4-DIONE;AVANDIA;ROSIGLITAZONE;ROSIGLITAZONE HCL;ROSIGLITAZONE HYDROCHLORIDE;Rosiglitazone free base;Rosiglitazone and its intermediates;5-[4-[2-(N-Methyl-N-(2-pyridyl)amino)ethoxy]benzylidine]-2,4-thiazolidinedione;5-[[4-[2-(methyl-pyridin-2-yl-amino)ethoxy]phenyl]methyl]thiazolidine-2,4-dione;BRL 49653;ROEIGLITAZONEMALEATE;CHEM-2353;2,4-Thiazolidinedione, 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-;5-(4-(2-(Methyl(pyridin-2-yl)amino)ethoxy)-benzyl)thiazolidine-2,4-dione;Rosiglitazone base;Rosiglitazone(ROZ,BRL 49653);5-[[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]methyl]-1,3-thiazolidine-2,4-dione;BRL-49653;Maleate;5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione;5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]-phenyl]methyl]-2,4-thiazolidine-dione;[ "" ];ROSIGLIAZONE;roiglitazone;ROSIGLITAZONEHCL;ROSIGLITAZONE 99%;Rosiglitazone, >=98.5%;Rosiglizole;Rosiglitazone maleate;rosiglitazone (Avandia);BRL49653;rosiglitazonum;rosiglitazona;TDZ 01;Avandaryl;Rosiglitazone [INN:BAN];Avandamet;Rosigilitazone;5-((4-(2-Methyl-2-(pyridinylamino)ethoxy)phenyl)methyl)-2,4-thiazolidinedione-2-butenedioate;C18H19N3O3S;YASAKCUCGLMORW-UH

Cas No.

122320-73-4

分子式

C₁₈H₁₉N₃O₃S

分子量

357.43

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

性状

Solid

IC50 & Target[1][2]

PPARγ

40 nM (Kd)

PPARγ

60 nM (EC₅₀)

TRPC5

30 μM (EC₅₀)

TRPM3

体外研究(In Vitro)

Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes.
Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons.
Rosiglitazone (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner.
Rosiglitazone (0.01-100 μM, 15 min) inhibits TRPM3 with IC₅₀ values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively.
Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation.
Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162)?induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells.

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

Cell Proliferation Assay

Cell Line:	A2780 and SKOV3 cells
Concentration:	0.5-50 μM
Incubation Time:	1-7 days
Result:	Inhibited cell proliferation in a time?dependent and concentration?dependent manner.

Western Blot Analysis

Cell Line:	Hippocampal neurons
Concentration:	1 μM
Incubation Time:	24 h
Result:	Increased NF-α1 and BCL-2 protein level.

体内研究(In Vivo)

Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats.
Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats.
Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models.

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

Animal Model:	Streptozotocin (STZ)-induced diabetic rats
Dosage:	5 mg/kg
Administration:	Oral administration, daily for 8 weeks.
Result:	Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group. Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups.

Animal Model:	Male Wistar rats
Dosage:	3 mg/kg/day
Administration:	Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks
Result:	Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS). Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. [Information]

[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. [Information]

[3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [Information]

[4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. [Information]

[5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. [Information]

[6]. Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. [Information]

[7]. Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85(2):273-284. [Information]

溶解度数据

体外研究:

DMSO : 250 mg/mL (699.44 mM; Need ultrasonic)

Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7978 mL	13.9888 mL	27.9775 mL
5 mM	0.5596 mL	2.7978 mL	5.5955 mL
10 mM	0.2798 mL	1.3989 mL	2.7978 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。-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 90% corn oil
Solubility: 2.5 mg/mL (6.99 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.99 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
2.

建议依照次序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution
3.

建议依照次序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution
4.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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
5.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.82 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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

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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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