SKL1223
SKL1223 is an orally effective thioredoxin-interacting protein (TXNIP) inhibitor with an IC50 of 0.64 µM. SKL1223 interacts with the E-box region of the TXNIP promoter to inhibit TXNIP transcription and related signaling pathways. SKL1223 reduces hepatic glucose output. SKL1223 exerts hypoglycemic effects by regulating the action of glucagon, and modulates blood glucose levels in Streptozotocin (HY-13753)-induced and obesity-induced diabetic mice. SKL1223 can be used in the research of type 1 diabetes and type 2 diabetes.
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- CAS 番号: 3093938-66-7
- 分子式: C19H15N3O2
- 分子量:317.34
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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生物活性
SKL1223 (10-20 μM; 24 h) significantly downregulates TXNIP mRNA expression in rat INS-1 cells and NES2Y cells, with dose-dependent downregulation confirmed by RNA-sequencing in rat INS-1 cells[1].
SKL1223 (0.2-25 μM; 24 h) dose-dependently reduces TXNIP protein expression in rat INS-1 cells, NES2Y cells, αTC1-6 cells, and primary mouse hepatocytes, with reduced protein levels confirmed by confocal microscopy in rat INS-1 cells[1].
SKL1223 (5-20 μM; 24 h) dose-dependently reduces basal glucagon secretion in αTC1-6 cells without altering intracellular glucagon content, with no effect on stimulated secretion from arginine + norepinephrine or low glucose conditions[1].
SKL1223 (5-20 μM; 6-24 h) suppresses glucagon-induced gluconeogenic gene expression, glucose output, and cAMP production in wild-type primary mouse hepatocytes, with the glucose output and cAMP effects independent of TXNIP but dependent on the glucagon receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:rat INS-1 cells, NES2Y cells
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Concentration:10 μM (qRT-PCR in INS-1 and NES2Y cells); 10-20 μM (RNA-sequencing in INS-1 cells)
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Incubation Time:24 h
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Result:Significantly reduced TXNIP mRNA expression in rat INS-1 cells and NES2Y cells.
Confirmed dose-dependent downregulation of the TXNIP gene in rat INS-1 cells via RNA-sequencing, with corresponding reduction in TXNIP protein generation.
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Cell Line:rat INS-1 cells, NES2Y cells, αTC1-6 mouse insulinoma alpha cells, primary mouse hepatocytes
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Concentration:0.2, 0.4, 0.8, 1.6, 3.2, 6.25, 12.5 and 25 μM
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Incubation Time:24 h
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Result:Caused a dose-dependent reduction in TXNIP protein expression in all tested cell types.
Showed a significant reduction in green fluorescent-labeled TXNIP protein in rat INS-1 cells via confocal microscopy.
SKL1223 (p.o.) improves glucose homeostasis in STZ-induced type 1 diabetic male C57BL/6J mice by reducing serum glucagon levels, lowering blood and urine glucose, and preserving pancreatic beta-cell function, with greater efficacy than standard oral anti-diabetic drugs[1].
SKL1223 (p.o.; 4 weeks) improves glucose homeostasis in obese, leptin receptor-deficient type 2 diabetic db/db mice by reducing serum glucagon levels, lowering blood glucose, and ameliorating hepatic steatosis, without altering body weight or insulin levels[1].
SKL1223 (70 mg/kg; p.o.; daily; 14 days) does not alter glucose homeostasis in TXNIP knockout male C57BL/6J mice, but causes a marginal increase in fasting serum glucagon levels, confirming its glucose-regulating effects are TXNIP-dependent[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J TXNIP-/- (8-week-old male; TXNIP deficiency)[1]
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Dosage:70 mg/kg
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Administration:p.o.; daily; 14 days
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Result:Showed no significant change in body weight compared to untreated TXNIP-/- controls.
Exhibited no significant difference in non-fasting blood glucose levels, unaffected glucose tolerance, and unchanged fasting blood glucose levels.
Caused a marginal increase in fasting serum glucagon levels compared to controls.
化学情報
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CAS 番号 3093938-66-7
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性状 Solid
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分子量 317.34
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分子式 C19H15N3O2
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Color White to off-white
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SMILES
C1(NCC2=CC=CO2)=CC=C(C=C1)C3=NC(C4=CC=CC=C4)=NO3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
SKL1223 関連分類
HY-181335 関連分類
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