| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
FK-614 (FK614; Tx-08-001; ATx-08001) is an insulin sensitizer and PPARγ modulator (SPPARM) with the potential to be used for treatment of postherpetic neuralgia, hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes. FK-614 is also a selective PPAR/peroxisome proliferator-activated receptor gamma agonist that improves peripheral glucose utilization while decreasing hepatic insulin extraction in alloxan-induced diabetic dogs.
| 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].
|
|---|---|
| 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].
|
| 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. |
| References |
|
| Additional Infomation |
FK614 has been used in trials studying the treatment of Diabetes Mellitus.
|
| Molecular Formula |
C21H23CL2N3O3S
|
|---|---|
| Molecular Weight |
468.393
|
| Exact Mass |
467.084
|
| CAS # |
193012-35-0
|
| PubChem CID |
9869229
|
| Appearance |
White to off-white solid powder
|
| LogP |
6.605
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
30
|
| Complexity |
688
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
UYGZODVVDUIDDQ-UHFFFAOYSA-N
|
| 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)
|
| Chemical Name |
3-[(2,4-dichlorophenyl)methyl]-2-methyl-N-pentylsulfonylbenzimidazole-5-carboxamide
|
| Synonyms |
FK614 ATx-08-001 FK 614 ATx-08001FK-614
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~213.49 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
