5.38439

RV1088

• Synonym(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
• Empirical Formula (Hill Notation): C₃₃H₃₄N₆O₄
• CAS Number: 1229606-73-8
• Molecular Weight: 578.66
• UNSPSC Code: 12352200

Properties

• Assay: ≥95% (HPLC)
• Quality Level: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pink-brown
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

General description

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.

Biochem/physiol Actions

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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

Legal Information

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

Safety Information

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