1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
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  3. Chiglitazar

Chiglitazar  (Synonyms: Carfloglitazar)

製品番号: HY-106266 純度: 99.70%
COA 取扱説明書 Technical Support

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

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Chiglitazar

Chiglitazar 構造式

CAS 番号 : 743438-45-1

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 378 在庫あり
Solution
10 mM * 1 mL in DMSO USD 378 在庫あり
Solid
5 mg $300 在庫あり
10 mg $490 在庫あり
25 mg $980 在庫あり
50 mg $1500 在庫あり
100 mg $2400 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of Chiglitazar:

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PPAR アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

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)

体外実験

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].

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

体内実験

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].

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

臨床実験
分子量

572.62

分子式

C36H29FN2O4

CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=C(F)C=C1)C(C=CC=C2)=C2N[C@H](C(O)=O)CC(C=C3)=CC=C3OCCN4C5=CC=CC=C5C6=CC=CC=C46

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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)

溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (174.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

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体積 (開始)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.81%

参考文献
動物実験
[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].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7464 mL 8.7318 mL 17.4636 mL 43.6590 mL
5 mM 0.3493 mL 1.7464 mL 3.4927 mL 8.7318 mL
10 mM 0.1746 mL 0.8732 mL 1.7464 mL 4.3659 mL
15 mM 0.1164 mL 0.5821 mL 1.1642 mL 2.9106 mL
20 mM 0.0873 mL 0.4366 mL 0.8732 mL 2.1829 mL
25 mM 0.0699 mL 0.3493 mL 0.6985 mL 1.7464 mL
30 mM 0.0582 mL 0.2911 mL 0.5821 mL 1.4553 mL
40 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0915 mL
50 mM 0.0349 mL 0.1746 mL 0.3493 mL 0.8732 mL
60 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7276 mL
80 mM 0.0218 mL 0.1091 mL 0.2183 mL 0.5457 mL
100 mM 0.0175 mL 0.0873 mL 0.1746 mL 0.4366 mL
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  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます:C1V1 = C2V2

濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
× = ×
C1   V1   C2   V2
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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製品名:
Chiglitazar
製品番号:
HY-106266
数量:
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