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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 97.02%
- 分子式: C42H57N7O9
- 分子量:803.94
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 6bK formate
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生物活性
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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.
化学情報
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性状 Solid
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分子量 803.94
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
6bK formate 関連分類
HY-110197A 関連分類
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