5.34377

CMB-087229

• Synonym(e): CMB-087229, 5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
• Empirische Formel (Hill-System): C₁₀H₈Cl₂N₂O₂
• CAS-Nummer: 1227692-67-2
• Molekulargewicht: 259.09
• MDL-Nummer: MFCD31745789
• UNSPSC-Code: 12352200
• PubChem Substanz-ID: 45102767
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Qualitätsniveau: 100
• Form: solid
• Hersteller/Markenname: Calbiochem^®
• Lagerbedingungen: OK to freeze; protect from light
• Farbe: white
• Löslichkeit: DMSO: 50 mg/mL
• Lagertemp.: 2-8°C
• SMILES String: C1=C(C=C(C=C1Cl)Cl)OCC2=CC(=O)NN2

Beschreibung

Allgemeine Beschreibung

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 (T_1/2 = 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.

Biochem./physiol. Wirkung

Cell permeable: yes

Primary Target
26S proteasome PSMC1 and PSMC4 and the chaperone protein TCP-1

Reversible: yes

Verpackung

Packaged under inert gas

Warnhinweis

Toxicity: Standard Handling (A)

Rekonstituierung

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sonstige Hinweise

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

Rechtliche Hinweise

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable