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Rosiglitazone maleate.

PPARγ激动剂，有效的胰岛素敏化剂,Rosiglitazone maleate 是一种有效的，选择性的 PPARγ 激活剂，对 PPARγ1，PPARγ2 和 PPARγ 的 EC50 值分别为 30 nM，100 nM 和 60 nM，对 PPARγ 的 Kd 值约为 40 nM；Rosiglitazone maleate 同时为 TRP channels 的调节剂，可抑制 TRPM2, TRPM3 的活性，激活 TRPC5。

目录号: PC12473 纯度: ≥98%

CAS No. :155141-29-0

商品编号	规格	价格	会员价
PC12473-25mg	25mg	¥490.00	请登录
PC12473-100mg	100mg	¥686.00	请登录
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PC12473-10mM (in 1mL DMSO)	10mM(in1mLDMSO)	¥490.00	请登录

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中文名称	Rosiglitazone maleate.
中文别名	马来酸罗格列酮;马来酸罗格利酮;罗格列酮马来酸盐;夫西地酸;邻氯苯基苄基酮;罗格列酮-D3;马来酸罗格列酮标准品;瑞格列奈;5-[4-[2-[N-甲基-N-(2-吡啶基)氨基]-乙氧基]苄基]噻唑烷-2,4二酮马来酸盐;矮牵牛素葡萄糖苷;马来酸罗格列酮(标准品);马来酸罗格列酮溶液,100PPM;罗格列酮马来酸盐；马来酸罗格利酮;马来酸罗格列酮溶液,1000PPM;马来酸罗格列酮；5-[4-[2-[N-甲基-N-(2-吡啶基)氨基]-乙氧基]苄基]噻唑烷-2,4二酮马来酸盐；罗格列酮马来酸盐；马来酸罗格利酮;罗格列酮马来酸盐、马来酸罗格利酮;马来酸罗格列酮(5-[4-[2-[N-甲基-N-(2-吡啶基)氨基]-乙氧基]苄基]噻唑烷-2,4二酮马来酸盐、罗格列酮马来酸盐、马来酸罗格利酮)
英文名称	Rosiglitazone maleate
英文别名	Rosiglitazone Maleate;Avandi;BRL-49653c;RSIGLITAZONEMALEATE;RosiglitazoneTartrate;Rosiglitazone Maleate (200 mg);5-{p-[2-(methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedione maleate;5-(4-(2-(Methyl(pyridin-2-yl)aMino)ethoxy)benzyl)thiazolidine-2,4-dione Maleate;5-((4-[2-(METHYL-2-PYRIDINYLAMINO)-ETHOXY]-PHENYL)-METHYLENE)-2,4-THIAZOLIDINEDIONE;5-[[4-[2-(Methyl-2-pyridinylaMino)ethoxy]phenyl]Methyl]-2,4-thiazolidinedione (2Z)-2-Butenedioate;2,4-Thiazolidinedione, 5-[[4-[2-(methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-, (2Z)-2-butenedioate (1:1);BRL 49653C;Rosiglitazone Maleate (BRL 49653C, Avandia®);Rosiglitazone-d3 Maleate;5-[[4-[2-(Methyl-2-pyridinylamino)ethoxy]phenyl]methyl]-2,4-thiazolidinedione maleate salt;Rosiglitazone Maleate forM;Rosiglitazone maleate Solution, 1000ppm;Avandia;Rosiglitazone (maleate);Rosiglitazone Maleate [USAN];BRL 49653-C;Avandamet;(+-)-5-(p-(2-(Methyl-2-pyridylamino)ethoxy)benzyl)-2,4-thiazolidinedione maleate (1:1);Nyracta;Rosiglitazone XR;2,4-Thiazolidinedione, 5-((4-(2-(methyl-2-pyridinylamino)ethoxy)phenyl)methyl)-, (2Z)-2-butenedioate (1:1);Venvia;SMR000471612;(Z)-but-2-enedioic
Cas No.	155141-29-0
分子式	C₂₂H₂₃N₃O₇S
分子量	473.50
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a K_d of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

性状

Solid

IC50 & Target[1][2]

PPARγ1

30 nM (EC₅₀)

PPARγ2

100 nM (EC₅₀)

体外研究(In Vitro)

Rosiglitazone maleate is a potent and selective activator of PPARγ, with EC₅₀s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a K_d of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes. Rosiglitazone (Compound 6) activates PPARγ, with an EC₅₀ of 60 nM. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner. Rosiglitazone completely inhibits TRPM3 with IC₅₀ values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC₅₀ of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC₅₀ of ～30 μM.

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

体内研究(In Vivo)

Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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]

溶解度数据

体外研究:

DMSO : 100 mg/mL (211.19 mM; Need ultrasonic)

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	2.1119 mL	10.5597 mL	21.1193 mL
5 mM	0.4224 mL	2.1119 mL	4.2239 mL
10 mM	0.2112 mL	1.0560 mL	2.1119 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 (sealed storage, away from moisture)。-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: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。
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 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: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 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 25.0 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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产品使用指南

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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