5.34377

CMB-087229

• 동의어(들): CMB-087229, 5-[(3,5-Dichlorophenoxy)methyl]-1,2-dihydro-3H-pyrazol-3-one, CMB087229
• 실험식(Hill 표기법): C₁₀H₈Cl₂N₂O₂
• CAS Number: 1227692-67-2
• Molecular Weight: 259.09
• MDL number: MFCD31745789
• UNSPSC 코드: 12352200
• PubChem Substance ID: 45102767
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C
• SMILES string: C1=C(C=C(C=C1Cl)Cl)OCC2=CC(=O)NN2

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

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

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable