1. Cell Cycle/DNA Damage
  2. PPAR
  3. Chiglitazar

Chiglitazar (Synonyms: Carfloglitazar)

目录号: HY-106266 纯度: 96.66%
产品使用指南

Chiglitazar (Carfloglitazar) 是泛过氧化物酶体增殖物激活受体 (PPARα/γ) 的双抑制剂,其对PPARα,PPARγ 和 PPARδ 的 EC50 值分别为 1.2,0.08 和 1.7 μM。

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Chiglitazar Chemical Structure

Chiglitazar Chemical Structure

CAS No. : 743438-45-1

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查看 PPAR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

IC50 & Target[1][2]

PPARα

1.8 μM (EC50)

PPARγ

0.08 μM (EC50)

PPARδ

1.7 μM (EC50)

体外研究
(In Vitro)

Comparative dose-response study of Chiglitazar is performed with rosiglitazone and pioglitazone for PPARγ, and WY14643 for PPARα. Chiglitazar shows significant activation of both the isoforms. Chiglitazar shows weaker PPARγ activating activity than rosiglitazone, but stronger than pioglitazone. In terms of PPARα activation, Chiglitazar shows more potent activity than rosiglitazone, pioglitazone, or WY14643 which is a selective PPARα agonist[1].

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

体内研究
(In Vivo)

After insulin injection, plasma glucose levels in the MSG rats treated with Chiglitazar or rosiglitazone are significantly reduced compared with the control group treated with vehicle at all time points. Fasting PI levels are lower in animals treated with Chiglitazar and rosiglitazone than control. The ISIs of MSG obese rats treated with chiglitazar and rosiglitazone are significantly higher than control. Furthermore, Chiglitazar ameliorates the HOMA indices. For IPGTT, at the 30 min after glucose loading, the glucose values in the 5 and 10 mg /kg Chiglitazar and rosiglitazone-treatment groups are significantly lower than those in the vehicle treatment group. The integrated for the glucose response during the IPGTT in the treatment groups are significantly less than those in the control groups[1].

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

Clinical Trial
分子量

572.62

Formula

C36H29FN2O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
In Vitro: 

DMSO : 100 mg/mL (174.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7464 mL 8.7318 mL 17.4636 mL
5 mM 0.3493 mL 1.7464 mL 3.4927 mL
10 mM 0.1746 mL 0.8732 mL 1.7464 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 (sealed storage, away from moisture and light)。-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 (4.37 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.37 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 ddH₂O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Animal Administration
[1]

Rats[1]
MSG obese rats (6 months old) are sorted into five treatment groups (n=10 each, male and female in half) based on decreased blood glucose in the insulin tolerance test, glucose levels, blood total triglyceride (TG), total cholesterol (TCHO), and initial body weight. From the next day, MSG obese rats receive single daily oral treatment with Chiglitazar (5, 10, and 20 mg kg-1 day-1, respectively), rosiglitazone (5 mg kg-1 day-1) or vehicle (water, 0.05% Tween 80) for 40 days. Normal wistar rats (n=10) serve as a normal group are treated with vehicle[1].

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

参考文献
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