Art. -Nr.: HY-101292

FK614

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FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.

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Reinheit: 99.97%
CAS. Nr.: 193012-35-0
Formel: C₂₁H₂₃Cl₂N₃O₃S
Molecular Weight:468.40

Speicherung:

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

FK614 Chemical Structure

CAS. Nr.: 193012-35-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PPAR-γ

Alle PPAR Isoform-spezifische Produkte anzeigen :

In Vitro

FK614 (0.1~10000 nM; 24 hours; CV-1 cells) activates PPARγ-dependent transcription in a concentration-dependent manner. FK614 (0~0.1 μM; 5 days; 3T3-L1 adipocytes) makes triglyceride content increased in a concentration-dependent manner. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation^[1].
FK614 is an insulin sensitizer potentially for treatment of postherpetic neuralgia. FK614 is a non-TZD insulin sensitizer^[2].

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

In Vivo

FK614 (0.32~3.2 mg/kg; p.o.; 14 days) dose-dependently reduces plasma glucose level^[3].
FK614 (0.1~10 mg/kg; p.o.; 14 days) improves the impaired glucose tolerance^[3].

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

Animal Model:

db/db Mice
Dosage:

0.1~10 mg/kg
Administration:

P.o.
Result:

Improved the impaired glucose tolerance.

Animal Model:

db/db Mice
Dosage:

0.32~3.2 mg/kg
Administration:

P.o.
Result:

Dose-dependently reduced plasma glucose level.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 193012-35-0
Appearance Solid
Molecular Weight 468.40
Formel C₂₁H₂₃Cl₂N₃O₃S
Color White to off-white
SMILES

O=C(C1=CC=C2N=C(C)N(CC3=CC=C(Cl)C=C3Cl)C2=C1)NS(=O)(CCCCC)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (213.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1349 mL

10.6746 mL

21.3493 mL

5 mM

0.4270 mL

2.1349 mL

4.2699 mL

10 mM

0.2135 mL

1.0675 mL

2.1349 mL

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fujimura T, et al. A selective peroxisome proliferator-activated receptor gamma modulator with distinct fat cell regulation properties. J Pharmacol Exp Ther. 2006;318(2):863-871. [Content Brief]

[2]. Fujimura T, et al. FK614, a novel peroxisome proliferator-activated receptor gamma modulator, induces differential transactivation through a unique ligand-specific interaction with transcriptional coactivators. J Pharmacol Sci. 2005;99(4):342-352. [Content Brief]

[3]. Minoura H, et al. Ameliorating effect of FK614, a novel nonthiazolidinedione peroxisome proliferator-activated receptor gamma agonist, on insulin resistance in Zucker fatty rat. Eur J Pharmacol. 2005;519(1-2):182-190. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	2.1349 mL	10.6746 mL	21.3493 mL	53.3732 mL
	5 mM	0.4270 mL	2.1349 mL	4.2699 mL	10.6746 mL
	10 mM	0.2135 mL	1.0675 mL	2.1349 mL	5.3373 mL
	15 mM	0.1423 mL	0.7116 mL	1.4233 mL	3.5582 mL
	20 mM	0.1067 mL	0.5337 mL	1.0675 mL	2.6687 mL
	25 mM	0.0854 mL	0.4270 mL	0.8540 mL	2.1349 mL
	30 mM	0.0712 mL	0.3558 mL	0.7116 mL	1.7791 mL
	40 mM	0.0534 mL	0.2669 mL	0.5337 mL	1.3343 mL
	50 mM	0.0427 mL	0.2135 mL	0.4270 mL	1.0675 mL
	60 mM	0.0356 mL	0.1779 mL	0.3558 mL	0.8896 mL
	80 mM	0.0267 mL	0.1334 mL	0.2669 mL	0.6672 mL
	100 mM	0.0213 mL	0.1067 mL	0.2135 mL	0.5337 mL

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FK614

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

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Highly Selective Activators Library

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MCE Bioactive Compound Library

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Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FK614

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Orally Active Compound Library

Anti-Obesity Compound Library

Transcription Factor-Targeted Library

Lipid Metabolism Compound Library

Antidepressant Compound Library

Human Metabolite Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Cancer Stem Cells Compound Library

Mitochondrial Protection Compound Library

Metabolic Enzyme Compound Library

Highly Selective Activators Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Cell Cycle/DNA Damage Compound Library

Metabolism/Protease Compound Library

Alle PPAR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

FK614 Related Classifications

HY-101292 Related Classifications