Rosiglitazone maleate - CAS:155141-29-0

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Rosiglitazone maleate (Synonyms:马来酸罗格列酮; BRL 49653C)

目录号 : KM4215 CAS No. : 155141-29-0 纯度 : 98%

Data Sheet 产品使用指南

Rosiglitazone maleate (BRL 49653C) 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 K_d 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。

规格	价格	是否有货
50mg		In-stock
200mg		In-stock
500mg	询价	In-stock
1g	询价	In-stock

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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).

体外研究

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.

体内研究

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.

分子式

C₂₂H₂₃N₃O₇S

分子量

473.50

CAS号

155141-29-0

中文名称

马来酸罗格列酮

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

溶解性数据

In Vitro:

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

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

配制储备液

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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.

请依序添加每种溶剂： 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。
2.

请依序添加每种溶剂： 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。
3.

请依序添加每种溶剂： 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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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KKL 顾客使用本产品发表的 33 篇科研文献

The molarity calculator equation

The dilution calculator equation