5.05981

PK11195

• 別名: PK11195, TSPO Activator II, Mitochondrial Translocator Protein Activator II, PK 11195, PK-11195, PK11195
• 実験式（ヒル表記法）: C₂₁H₂₁ClN₂O
• CAS番号: 85532-75-8
• 分子量: 352.86
• MDL番号: MFCD00069334
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: solid
• 有効性: 20 nM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 100 mM
• 保管温度: 2-8°C
• SMILES記法: Clc1c(cccc1)c2nc(cc3c2cccc3)C(=O)N(C(CC)C)C
• InChI: 1S/C21H21ClN2O/c1-4-14(2)24(3)21(25)19-13-15-9-5-6-10-16(15)20(23-19)17-11-7-8-12-18(17)22/h5-14H,4H2,1-3H3
• InChI Key: RAVIZVQZGXBOQO-UHFFFAOYSA-N

詳細

詳細

An isoquinoline carboxamide that acts as a potent ligand for peripheral bezodiazepine receptor (K_d = 20 nM). Exhibits anti-inflammatory properties. Binds to monocytes and following lesioning its binding up-regulated in brain macrophages and activated microglia. Shown to enhance the susceptibility of cells to apoptosis induction by DNA damaging agents and can reverse the suppression of apoptosis by Bcl-2. Serves as a ligand of the outer membrane translocator protein and reduces mitochondrial transmembrane potential within 30 minutes of exposure (˜100 µM).

生物化学的／生理学的作用

Primary Target
peripheral bezodiazepine receptor

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

Naoi, M., et al., 2013. J. Neural Transm.In press
Casellas, P., et al., 2002. Neurochem. Int.40, 475.

Waterfield, J.D., et al., 1999. Rheumtology38, 1068.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable