RAGE406R
RAGE406R is an orally active RAGE-DIAPH1 interaction antagonist. RAGE406R can bind to ctRAGE and prevent the formation of the RAGE-DIAPH1 complex and inhibit its interaction. RAGE406R can reduce the expression of CCL2, TNF, and IL-6 in THP1 cells. RAGE406R suppresses delayed-type hypersensitivity in T2D mice. RAGE406R can be used for the study of diabetes.
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- No. CAS: 3034560-21-6
- Fòrmula: C25H24N4O2
- Peso molecular:412.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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IL-6 |
RAGE406R (8.1 nM) inhibits the activation of DIAPH1 actin polymerization activity by ctRAGE by antagonizing the interaction between ctRAGE and DIAPH1[1].
RAGE406R (0.1-5.0 μM, 1 h) dose-dependently reduces the intracellular proximity of RAGE and DIAPH1. After adding 0.1 μM RAGE406R, the FRET efficiency decreases to 4.7 %; at 5.0 μM, it decreased to 1.6 %[1].
RAGE406R (0.00006-10 μM, 1.5 h) increases the inhibition of RAGE ligand-stimulated SMC migration, with an IC50 of 2 nM in murine aortic SMCs[1].
RAGE406R (10 μM, 1.5 h) significantly reduces the expression of CCL2, TNF, and IL-6 in THP1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Primary murine aortic SMCs
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Concentration:0.00006 μM, 0.0002 μM, 0.001 μM, 0.002 μM, 0.005 μM, 0.014 μM, 0.041 μM, 0.123 μM, 0.370 μM, 1.111 μM, 3.333 μM, 10 μM
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Incubation Time:1.5 h
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Result:Increased the inhibition of RAGE ligand-stimulated SMC migration, with an IC50 of 2 nM in murine aortic SMCs.
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Cell Line:THP1 cells
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Concentration:10 μM
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Incubation Time:1.5 h
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Result:Significantly reduced the expression of CCL2, TNF, and IL6 in THP1 cells.
RAGE406R (5 mg/kg, topical application, twice daily for 8 days) accelerates the healing of diabetic wounds in mice and has a more comprehensive anti-inflammatory effect in males[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CF-1 mice were immunosensitized by injection of methylated bovine serum albumin (mBSA) (immunogen being mBSA + Freund's incomplete adjuvant emulsion) into the left inguinal lymph node. Three weeks later, an inflammatory response was elicited by injection of mBSA (20 μg) into the left hind paw pad[1].
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Dosage:5 mg/kg
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Administration:P.o., twice daily (12-hour intervals) for a total of 4 doses
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Result:Inflammation score significantly reduced.
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Animal Model:Full-thickness 1 cm × 1 cm excisional wounds were created on the backs of male and female mouse models of T2D, ob/ob mice; wounds were covered with Tegaderm clear dressing[1].
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Dosage:5 mg/kg
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Administration:Topical application, twice daily for 8 days
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Result:Significantly promoted wound closure.
Inflammation was reduced, collagen deposition increased, and epithelial migration accelerated.
In male mice, the expression of Ccl2, TNF, and IL-6 was significantly reduced; in female mice, only Ccl2 expression was significantly decreased, while TNF and IL-6 showed no significant changes.
Chemical Information
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No. CAS 3034560-21-6
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Peso molecular 412.48
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Fòrmula C25H24N4O2
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SMILES
N#CC1=CC=C2C(CN3CCOCC3)=CC(C4=CC=C(C=C4)[C@H]5CCC(N5)=O)=NC2=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RAGE406R Related Classifications
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