5.32583

TLR1/TLR2 Agonist II, CU-T12-9

• Synonyme(s) : TLR1/TLR2 Agonist II, CU-T12-9, N-Methyl-4-nitro-2-(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-1-yl)aniline, CUT129
• Formule empirique (notation de Hill): C₁₇H₁₃F₃N₄O₂
• Numéro CAS: 1821387-73-8
• Poids moléculaire : 362.31
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: powder
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: yellow
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

A diphenyl substituted imidazole based compound that directly and selectively targets TLR1/2 and induces their dimerization and activates TLR1 & 2 signaling leading to NF-κB and AP-1 activation (K_D = 182 and 478 nM, respectively; EC₅₀ = 52.9 nM for TLR2 in HEK-Blue cells over-expressing hTLR2). Does not affect the dimerization of TLR2/TLR6 and exhibits poor affinity towards TLR3, TLR4, TLR5, TLR7 and TLR8. Shown to compete with Pam₃CSK₄ (Cat. No. 506350; K_i = 45.4 nM) for binding to TLR1/2 interface and enhance heterodimerization. Up-regulates the expression of TLR1, TLR2, TNFα, IL-10, and iNOS in RAW 264.7 macrophages in a time-dependent manner. Shown to be non-toxic up to 100 µM concentration.

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

A non-cytotoxic (up to 100 µM) diphenyl-substituted imidazole compound that exhibits high affinity toward both TLR1 & TLR2 (K_D = 182 nM & 478 nM, respectively) and induces TLR1/2 heterodimerization, effectively completing against Pam₃CSK₄ (Cat. No. 506350) for TLR1/2 binding (K_i = 45.4 nM; [Pam3] = 20 mg/mL; [TLR1/2] = 80 nM). Shown to potently induce secreted embryonic alkaline phosphatase (SEAP) production from human TLR2-, but not TLR3-, 4-, 5-, 7-, 8-, transfected HEK293 (EC₅₀ = 52.9 nM) in an NF-κB inhibitor Triptolide-(Cat. No. 645900) blockable manner via selective TLR1/2, but not TLR2/6, heterodimer activation. Reported to induce comparable NF-κB-dependent reporter transcription as 100 ng/mL Pam₃CSK₄ when administered to human macrophage U937 cultures at 5 µM concentration (24 h) and effectively trigger NO production in both murine Raw 264.7 and primary rat macrophage cultures (EC_max = 1.2 & 0.4 µM, respectively; 24 h), blockable by TLR1/2 antagonist CU-CPT22 (Cat. No. 614305), but not TLR4 antagonist TAK-242 (Cat. No. 614316 & 508336). Likewise, both CU-T12-9 and Pam₃CSK₄ (1 µM & 50 ng/mL, respectively) are demonstrated to induce similar time-dependent induction of TLR1, TLR2, TNF-α, iNOS, IL-10 mRNA in Raw 264.7 cells.

TLR1/TLR2 Agonist & CU-T12-9

Actions biochimiques/physiologiques

Primary Target
TLR1/TLR2

Reversible: yes

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

Cheng, K., et al. 2014. Manuscript in preparation.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable