5.34377
CMB-087229
Synonym(s):
CMB-087229, 5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
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About This Item
Empirical Formula (Hill Notation):
C10H8Cl2N2O2
CAS Number:
Molecular Weight:
259.09
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Recommended Products
Assay
≥98% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
SMILES string
C1=C(C=C(C=C1Cl)Cl)OCC2=CC(=O)NN2
General description
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.
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.
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1
26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Tripper, P.C., et al. 2014. ACS Chem. Neurosci.5, 823.
Chen, T., et al. 2012. J. Med. Chem.55, 515.
Chen, T., et al. 2012. J. Med. Chem.55, 515.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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