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534377 CMB-087229 - CAS 1227692-67-2 - Calbiochem

534377
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1227692-67-2C₁₀H₈Cl₂N₂O₂

Products

Catalogue NumberPackaging Qty/Pack
5.34377.0001 Glass bottle 25 mg
Description
OverviewA 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.
Catalogue Number534377
Brand Family Calbiochem®
Synonyms5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
References
ReferencesTripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
Chen, T., et al. 2012. J. Med. Chem. 55, 515.
Product Information
CAS number1227692-67-2
FormWhite solid
Hill FormulaC₁₀H₈Cl₂N₂O₂
Chemical formulaC₁₀H₈Cl₂N₂O₂
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary Target26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5.34377.0001 04054839117176

Documentation

CMB-087229 - CAS 1227692-67-2 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

CMB-087229 - CAS 1227692-67-2 - Calbiochem Certificates of Analysis

TitleLot Number
534377

References

Reference overview
Tripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
Chen, T., et al. 2012. J. Med. Chem. 55, 515.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision28-July-2017 JSW
Synonyms5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
DescriptionA 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number1227692-67-2
Chemical formulaC₁₀H₈Cl₂N₂O₂
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesTripper, P.C., et al. 2014. ACS Chem. Neurosci. 5, 823.
Chen, T., et al. 2012. J. Med. Chem. 55, 515.