5.08578

TSPO Agonist, Ro5-4864

• 別名: TSPO Agonist, Ro5-4864, 4ʹ-chlorodiazepam, TSPO Activator I, Mitochondrial Translocator Protein Activator I, Ro54864
• 実験式（ヒル表記法）: C₁₆H₁₂Cl₂N₂O
• CAS番号: 14439-61-3
• 分子量: 319.19
• MDL番号: MFCD00043406
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 4.4 nM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C
• InChI: 1S/C16H12Cl2N2O/c1-20-14-7-6-12(18)8-13(14)16(19-9-15(20)21)10-2-4-11(17)5-3-10/h2-8H,9H2,1H3
• InChI Key: PUMYFTJOWAJIKF-UHFFFAOYSA-N

詳細

詳細

A 4′-chloro derivative of diazepam that lacks affinity for GABA-A receptors, but can serve as a ligand for the peripheral benzodiazepine receptor. Acts as an agonist for the 18 kDa translocator protein (TSPO) on the outer mitochondrial membrane (K_d = 4.4 nM). Diminishes the accumulation of β-amyloid peptides in the CA1 hippocampal region of gonadectomized (GDX) mice and in triple transgenic Alzheimer′s disease murine models (3xTgAD). However, it does not affect tau phosphorylation events as assessed by AT8 immunoreactivity. Also shown to reduce GFAP ionized calcium binding adaptor molecule-1 (IBA-1) in the 3xTgAD mice. Reported to increase testosterone and progesterone levels in GDX mice without affecting other steroid hormones. However, it does not have a significant effect on the levels of these hormones in aged 3xTgAD mice. In combination with another mitochondria targeting molecule, lonidamine, it is shown to induce apoptosis in MDA-MB-231 breast cancer cells.

A 4′-chloro derivative of diazepam that lacks affinity for GABA-A receptors, but can serve as a ligand for the peripheral benzodiazepine receptor. Acts as an agonist for the 18 kDa translocator protein (TSPO) on the outer mitochondrial membrane (K_d = 4.4 nM). Diminishes the accumulation of β-amyloid peptides in the CA1 hippocampal region of gonadectomized (GDX) mice and in triple transgenic Alzheimer′s disease murine models (3xTgAD). However, it does not affect tau phosphorylation events as assessed by AT8 immunoreactivity. Also shown to reduce GFAP ionized calcium binding adaptor molecule-1 (IBA-1) in the 3xTgAD mice. Reported to increase testosterone and progesterone levels in GDX mice without affecting other steroid hormones. However, it does not have a significant effect on the levels of these hormones in aged 3xTgAD mice. In combination with another mitochondria targeting molecule, lonidamine, it is shown to induce apoptosis in MDA-MB-231 breast cancer cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
TSPO

包装

Packaged under inert gas

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

Barron, A.M., et al. 2013. The J.Neuroscience.33, 8891.Yousefi, O.S., et al. 2013. Cell Commun.Signaling.11, 13.Wu, X., and Gallo, K.E. 2013. PLoS One.8, e71258.Leonelli, E., et al. 2005. Mech. Ageing. Dev.126, 1159.

法的情報

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

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H302
• 注意書き: P264 - P270 - P301 + P312 - P501
• 危険有害性の分類: Acute Tox. 4 Oral
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable