5.38439

RV1088

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₃₃H₃₄N₆O₄
• Número CAS: 1229606-73-8
• Peso molecular: 578.66
• Código UNSPSC: 12352200

Propriedades

• Ensaio: ≥95% (HPLC)
• Nível de qualidade: 100
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: pink-brown
• solubilidade: DMSO: 100 mg/mL
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable