CMB-087229 – Calbiochem

Descrição detalhada : A cell-permeable, blood-brain barrier permeable, non-toxic pyrazolone compound that potently blocks mutant Cu/Zn SOD1 cytotoxicity (EC50 = 67 nM in PC12 cells expressing mutant G93A SOD1). Shown to directly interact with 26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1 and enhance proteasome activity. Offers neuroprotection against protein aggregation induced toxicity and prolongs the survival of ALS transgenic mice by 13.3% (20 mg/kg, i.p., q.d.) Demonstrates attractive microsomal (T1/2 = 93 & 36 min in human & mouse, respectively) and metabolic stability, aqueous solubility (250 µM) and PK profile in mice. Poorly affects the activities of 68-enzymes & receptors, hERG and Cyp450 isozymes at 10 µM.Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water., A cell-permeable, blood-brain barrier permeable, non-toxic pyrazolone compound that potently blocks mutant Cu/Zn SOD1 cytotoxicity (EC50 = 67 nM in PC12 cells expressing mutant G93A SOD1). Shown to directly interact with 26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1 and enhance proteasome activity. Offers neuroprotection against protein aggregation induced toxicity and prolongs the survival of ALS transgenic mice by 13.3% (20 mg/kg, i.p., q.d.) Demonstrates attractive microsomal (T1/2 = 93 & 36 min in human & mouse, respectively) and metabolic stability, aqueous solubility (250 µM) and PK profile in mice. Poorly affects the activities of 68-enzymes & receptors, hERG and Cyp450 isozymes at 10 µM.
Sinónimos : CMB-087229 - Calbiochem; 5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
Fórmula molecula r: C10H8Cl2N2O2
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA