407616

IL-1R Antagonist

The IL-1R Antagonist, also referenced under CAS 566914-00-9, controls the biological activity of IL-1R.

• Synonym(s): IL-1R Antagonist, BB-loop Mimic, Hydrocinnamoyl-L-valyl Pyrrolidine, TIR Domain Mimic
• Empirical Formula (Hill Notation): C₁₈H₂₆N₂O₂
• CAS Number: 566914-00-9
• Molecular Weight: 302.41
• MDL number: MFCD06411423
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥95% (HPLC)
• form: oil
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: colorless
• solubility: DMSO: 10 mg/mL; ethanol: soluble
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: N2(CCCC2)C(=O)[C@@H](NC(=O)CCc1ccccc1)C(C)C
• InChI: 1S/C18H26N2O2/c1-14(2)17(18(22)20-12-6-7-13-20)19-16(21)11-10-15-8-4-3-5-9-15/h3-5,8-9,14,17H,6-7,10-13H2,1-2H3,(H,19,21)/t17-/m0/s1
• InChI key: DAZSWUUAFHBCGE-KRWDZBQOSA-N

Description

General description

A cell-permeable, end protected L-valyl derivative modeled on the MyD88-binding sequence of the TIR (Toll/IL-1R/resistance) domain BB-loop of IL-1RI (type I IL-1 receptor). It specifically inhibits TIR domain-mediated MyD88/IL1-RI interaction without affecting TLR4/MyD88 interaction. It was used successfully to reduce IL-1β-induced fever in mice in vivo and to attenuate IL-1β-induced, but not LPS-induced, activation of MAP kinase signaling cascades in murine lymphocytes and EL4 thymoma cells in vitro.

A cell-permeable, end protected L-valyl derivative of the MyD88-binding sequence of the TIR (Toll/IL-1R/resistance) domain BB-loop of IL-1RI (type I IL-1 receptor). It specifically inhibits TIR domain-mediated MyD88/IL1-RI interaction without affecting TLR4/MyD88 interaction. It was used successfully to reduce IL-1β-induced fever in mice in vivo and to attenuate IL-1β-induced, but not LPS-induced, activation of MAP kinase signaling cascades in murine lymphocytes and EL4 thymoma cells in vitro.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
TIR domain-mediated MyD88/IL1-RI interaction

Product does not compete with ATP.

Reversible: no

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

Bartfai, T., et al. 2003. Proc. Natl. Acad. Sci. USA100, 7971.

Legal Information

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

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable