5.38439

RV1088

• 別名: RV1088, N-[4-[[4-[[[[3-(1,1-dimethylethyl)-1-(4-methylphenyl)-1H-pyrazol-5-yl]amino]carbonyl]amino]-1-naphthalenyl]oxy]-2-pyridinyl]-2-methoxyacetamide
• 実験式（ヒル表記法）: C₃₃H₃₄N₆O₄
• CAS番号: 1229606-73-8
• 分子量: 578.66
• UNSPSCコード: 12352200

特性

• アッセイ: ≥95% (HPLC)
• 品質水準: 100
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: pink-brown
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C

詳細

詳細

A cell-permeable, naphthalene based compound that acts as a narrow spectrum kinase inhibitor and reduces pro-inflammatory cytokine synthesis in LPS-activated primary human macrophages (IC₅₀ = 0.63 and 1.66 nM for TNFα and IL-6), monocytes (IC₅₀ = 0.97, 1.1, and 1.32 nM for TNFα, IL-6, and IL-8), and synovial fibroblasts (5.45 and 1.61 nM for IL-6 and IL-8). Shown to simultaneously inhibit the activity of p38α, p38γ, and Src (c-Src and Hck, and Syk). Also reported to inhibit antigen-induced release of beta-Hex, LTC4, and PGD2 (IC₅₀ = 18, 11, and 21 nM, respectively) in cord blood derived mast cells.

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
p-38α, p38γ, c-Src, Hck and SyK

Reversible: yes

Target IC₅₀: 5.45 nM, 1.61 nM for IL-6, IL-8 inhibition respectively in activated rheumatoid arthritis synovial fibroblasts

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

To, W. S., et al. 2015. Br. J. Pharmacol.172, 3805.

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