6bK formate
Based on 2 publication(s) in Google Scholar
6bK formate is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK formate 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 formate improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK formate can be used in research related to type 2 diabetes.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.02%
- Fòrmula: C42H57N7O9
- Peso molecular:803.94
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) 6bK formate
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Actividad biológica
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IDE 50 nM (IC50) |
6bK formate potently inhibits IDE activity with an IC50 of 50 nM[2].
6bK (1 h) formate 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) formate 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) formate 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.
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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]
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Dosage:40-90 mg/kg
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Administration:single injection
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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
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Appearance Solid
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Peso molecular 803.94
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Fòrmula C42H57N7O9
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Color White to off-white
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SMILES
O=CO.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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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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
Pureza y Documentación
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Ficha de datos (276 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
6bK formate Related Classifications
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