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| Targets |
FK-614 targets peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor involved in glucose and lipid metabolism. It acts as a selective PPARγ agonist. FK-614 is a non-thiazolidinedione (non-TZD) type PPARγ modulator with different effects on PPARγ activation at each stage of adipocyte differentiation.
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| ln Vitro |
In a concentration-dependent manner, FK614 (0.1~10000 nM; 24 hours; CV-1 cells) promotes PPARγ-dependent transcription. In a concentration-dependent manner, FK614 (0~0.1 μM) raised the triglyceride content in 3T3-L1 adipocytes after 5 days. At different phases of adipocyte development, FK614 affects PPARγ activation differently [1]. An insulin sensitizer called FK614 is used to treat postherpetic neuralgia. An insulin sensitizer that is not TZD is FK614 [2].
In vitro, FK-614 acts as a selective PPARγ agonist. It activates PPARγ with different effects at each stage of adipocyte differentiation. The compound promotes adipocyte differentiation and improves insulin sensitivity in cultured cells. Specific EC50 values for PPARγ activation are not extensively documented in publicly available literature. |
| ln Vivo |
A dose-dependent reduction in plasma glucose levels is observed with FK614 (0.32~3.2 mg/kg; oral; 14 days) [3]. The oral medication FK614 (0.1–10 mg/kg) is used for 14 days to treat impaired glucose tolerance [3].
In vivo, FK-614 improves peripheral glucose utilization while decreasing hepatic insulin extraction in alloxan-induced diabetic dogs. It has potent anti-diabetic activity and has been studied for the treatment of hyperglycemia, hypertriglyceridemia, glucose intolerance, and type 2 diabetes. The compound is an orally active insulin sensitizer. |
| Enzyme Assay |
The in vitro receptor binding assay for FK-614 involves measuring its affinity for peroxisome proliferator-activated receptor gamma (PPARγ). Radiolabeled ligand binding or fluorescence polarization assays are performed using recombinant PPARγ protein. Varying concentrations of FK-614 are incubated with the receptor, and binding affinity (IC50 or EC50) is determined. FK-614 acts as a selective PPARγ agonist.
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| Cell Assay |
In vitro cellular assays for FK-614 involve treating cultured adipocytes or other PPARγ-expressing cells with varying concentrations of the compound. Adipocyte differentiation is assessed by measuring lipid accumulation using Oil Red O staining. PPARγ target gene expression (e.g., adiponectin, aP2) is measured by qRT-PCR. Glucose uptake is assessed using radiolabeled 2-deoxyglucose. FK-614 activates PPARγ with different effects at each stage of adipocyte differentiation.
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| Animal Protocol |
Animal/Disease Models: db/db mouse
Doses: 0.1~10 mg/kg Route of Administration: Po Experimental Results:Improved impaired glucose tolerance. Animal/Disease Models: db/db mice Doses: 0.32~3.2 mg/kg Route of Administration: Po Experimental Results: Plasma glucose levels diminished in a dose-dependent manner. In vivo animal experiments for FK-614 typically use diabetic animal models such as alloxan-induced diabetic dogs or genetically diabetic rodents. FK-614 is administered orally at various doses. Blood glucose, insulin, and triglyceride levels are measured. Glucose tolerance tests are performed to assess peripheral glucose utilization. Hepatic insulin extraction is measured using catheterization techniques in dogs. |
| ADME/Pharmacokinetics |
FK-614 is an orally active compound. It has a molecular weight of 501.02 (C25H24Cl2N4O3S). As a small molecule PPARγ agonist, FK-614 is expected to have good oral bioavailability and extensive plasma protein binding. Specific PK parameters including half-life, Cmax, and metabolic pathways would be available from preclinical studies.
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| Toxicity/Toxicokinetics |
FK-614 has been studied for the treatment of type 2 diabetes and related metabolic disorders. As a PPARγ agonist, potential adverse effects may include weight gain, fluid retention, and edema, which are class effects of PPARγ agonists. The compound's non-TZD structure may offer a different safety profile compared to thiazolidinediones. Complete toxicology data would be available from preclinical development programs.
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| References |
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| Additional Infomation |
FK614 has been used in trials for diabetes treatment.
FK-614 (CAS#: 193012-35-0) is an orally active, non-thiazolidinedione selective PPARγ agonist and insulin sensitizer. It improves peripheral glucose utilization while decreasing hepatic insulin extraction in diabetic dogs. FK-614 has been studied for type 2 diabetes, hyperglycemia, and hypertriglyceridemia. The compound is not approved for clinical use and remains an investigational compound. |
| Molecular Formula |
C21H23CL2N3O3S
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| Molecular Weight |
468.393
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| Exact Mass |
467.084
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| CAS # |
193012-35-0
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| PubChem CID |
9869229
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| Appearance |
White to off-white solid powder
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| LogP |
6.605
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
30
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| Complexity |
688
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UYGZODVVDUIDDQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23Cl2N3O3S/c1-3-4-5-10-30(28,29)25-21(27)15-7-9-19-20(11-15)26(14(2)24-19)13-16-6-8-17(22)12-18(16)23/h6-9,11-12H,3-5,10,13H2,1-2H3,(H,25,27)
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| Chemical Name |
3-[(2,4-dichlorophenyl)methyl]-2-methyl-N-pentylsulfonylbenzimidazole-5-carboxamide
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| Synonyms |
FK614 ATx-08-001 FK 614 ATx-08001FK-614
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~213.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1350 mL | 10.6749 mL | 21.3497 mL | |
| 5 mM | 0.4270 mL | 2.1350 mL | 4.2699 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1350 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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