6bK TFA
Based on 2 publication(s) in Google Scholar
6bK TFA is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK TFA binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK TFA improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK TFA can be used in research related to type 2 diabetes.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.68%
- CAS No.: 1774353-12-6
- Formule: C43H56F3N7O9
- Masse moléculaire:871.94
-
Stockage:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) 6bK TFA
More
Activité biologique
|
IDE 50 nM (IC50) |
6bK TFA potently inhibits IDE activity with an IC50 of 50 nM[2].
6bK (1 h) TFA exhibits a high plasma protein binding rate, as well as favorable 1-hour stability in mouse plasma and microsomes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Acute inhibition of insulin-degrading enzyme by 6bK (40-90 mg/kg) TFA improves oral glucose tolerance in lean and DIO mice, delays gastric emptying via the amylin signaling pathway, impairs intraperitoneal glucose tolerance via the glucagon signaling pathway, and enhances insulin-mediated hypoglycemic responses, all of which depend on IDE activity[2].
6bK (80 mg/kg; i.p.; single administration) TFA exhibits a potentiated hypoglycemic response to insulin injection in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J mice (male; lean: 14-16 weeks old; diet-induced obese: 24-26 weeks old, >20 weeks on high-fat diet)[2]
-
Dosage:40-90 mg/kg
-
Administration:single injection
-
Result:Increased relative blood glucose profile areas during IPGTT.
Reduced relative blood glucose during the OGTT.
Showed stronger hypoglycaemic responses to insulin, stronger hyperglycaemic responses to amylin and glucagon.
Chemical Information
-
CAS No. 1774353-12-6
-
Appearance Solid
-
Masse moléculaire 871.94
-
Formule C43H56F3N7O9
-
Color White to off-white
-
SMILES
O=C(N[C@@H](C(NCCCC[C@H]1C(N)=O)=O)CC(C=C2)=CC=C2C(C3=CC=CC=C3)=O)[C@@H](NC([C@@H](NC(/C=C/C(N1)=O)=O)CCCCN)=O)CC4CCCCC4.OC(C(F)(F)F)=O
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
Mol Biomed
ML345 is a potent and selective NLRP3 inflammasome inhibitor with anti-inflammatory activity. [Abstract]2025 Nov 13;6(1):108. PMID: 41231359 -
Mol Med
Inhibition of insulin degrading enzyme suppresses osteoclast hyperactivity via enhancing Nrf2-dependent antioxidant response in glucocorticoid-induced osteonecrosis of the femoral head. [Abstract]2024 Jul 31;30(1):111. PMID: 39085816
Solvant et solubilité
DMSO : 100 mg/mL (114.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.87 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.87 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
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 (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (278 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Costes S, et al. Insulin-degrading enzyme inhibition, a novel therapy for type 2 diabetes?. Cell Metab. 2014;20(2):201-203. [Content Brief]
[2]. Maianti JP, et al. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones. Nature. 2014;511(7507):94-98. [Content Brief]
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 (protect from light, stored under nitrogen). 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 | 1.1469 mL | 5.7343 mL | 11.4687 mL | 28.6717 mL |
| 5 mM | 0.2294 mL | 1.1469 mL | 2.2937 mL | 5.7343 mL | |
| 10 mM | 0.1147 mL | 0.5734 mL | 1.1469 mL | 2.8672 mL | |
| 15 mM | 0.0765 mL | 0.3823 mL | 0.7646 mL | 1.9114 mL | |
| 20 mM | 0.0573 mL | 0.2867 mL | 0.5734 mL | 1.4336 mL | |
| 25 mM | 0.0459 mL | 0.2294 mL | 0.4587 mL | 1.1469 mL | |
| 30 mM | 0.0382 mL | 0.1911 mL | 0.3823 mL | 0.9557 mL | |
| 40 mM | 0.0287 mL | 0.1434 mL | 0.2867 mL | 0.7168 mL | |
| 50 mM | 0.0229 mL | 0.1147 mL | 0.2294 mL | 0.5734 mL | |
| 60 mM | 0.0191 mL | 0.0956 mL | 0.1911 mL | 0.4779 mL | |
| 80 mM | 0.0143 mL | 0.0717 mL | 0.1434 mL | 0.3584 mL | |
| 100 mM | 0.0115 mL | 0.0573 mL | 0.1147 mL | 0.2867 mL |
6bK TFA Related Classifications
HY-110197 Related Classifications
Powered by Bioz