SAR113945
SAR113945 is a highly selective IKK-β inhibitor with an IC50 value of 0.4 nM. SAR113945 blocks the canonical NFκB signaling pathway. SAR113945 alleviates hyperalgesia to heat and mechanical stimuli, and exerts effects in a zymosan-induced knee joint inflammation model. SAR113945 is applicable to research related to symptomatic knee osteoarthritis.
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- No. CAS: 869796-50-9
- Fòrmula: C28H25N7O3
- Peso molecular:507.55
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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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Chemical Information
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
IKK-β |
In Vitro
SAR113945 potently inhibits the native IKK complex purified from HeLa cell extracts, with an IC50 of 0.018 μM[1].
SAR113945 (10 μM) exhibits high kinase specificity. In a kinome panel comprising 62 kinases, it only inhibits mixed lineage kinase 1 (MLK1) by 59% at a concentration of 10 μM[1].
SAR113945 (10 μM) exhibits high receptor and enzyme specificity, acting solely as an antagonist of the adenosine A3 receptor, with an IC50 of 0.89 μM in a screening panel comprising 106 targets[1].
SAR113945 (Compound 1) inhibits IKK-β with an IC50 of 0.4 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Lewis rats (male)[1]
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Dosage:0.01 mg per joint; 0.1 mg per joint; 1 mg per joint; 10 mg per joint
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Administration:intra-articular; single dose
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Result:Produced a maximum pain reduction of 88% at the highest dose of 10 mg per joint.
Was well tolerated.
Chemical Information
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No. CAS 869796-50-9
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Peso molecular 507.55
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Fòrmula C28H25N7O3
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SMILES
N(C[C@H](NC(=O)C=1C=C2C(=CC1)NC(=C2)C3=NC(NC)=NC=C3)C(O)=O)(C4=CC=CC=C4)C5=CC=CC=N5
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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
[1]. Grothe K, et al. IκB kinase inhibition as a potential treatment of osteoarthritis - results of a clinical proof-of-concept study. Osteoarthritis Cartilage. 2017 Jan;25(1):46-52. [Content Brief]
[2]. Liu D, et al. Small molecule inhibitors of osteoarthritis: Current development and future perspective. Frontiers in physiology. 2023;14:1156913. [Content Brief]
[3]. Noha SM, et al. Discovery of a novel IKK-β inhibitor by ligand-based virtual screening techniques. Bioorganic & medicinal chemistry letters. 2011 Jan 01;21(1):577-83. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SAR113945 Related Classifications
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