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CL097

Cat. No.: ISPL-0247

For research use only. We do not sell to patients.

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CL097

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Biological activity

Description

CL097, a potent TLR7/8 agonist, induces pro-inflammatory cytokines in macrophages [1]. CL097 induces NADPH oxidase priming, resulting in an increase in the fMLF-stimulated ROS production. Highly water-soluble derivative of the imidazoquinoline compound R848 (Resiquimod)

In Vitro

CL097 induces activation of NF-κB at 0.1 μM in TLR7-transfected HEK293 cells and at 4 μM in TLR8-transfected HEK293 cells [1].
CL097 induces hyperactivation of the NADPH oxidase by stimulating the phosphorylation of p47phox on selective sites in human neutrophils and suggests that p38 MAPK, ERK1/2, protein kinase C, and Pin1 control this process. CL097 induces the phosphorylation of p47phox on specific sites and enhances fMLF-induced p47phox phosphorylation [2].

Innatura has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

CL097 and CD40 agonist stimulation induce efficient diabetogenic Cytotoxic T lymphocyte (CTL) function in NOD mice. CL097 (5 mg/kg, s.c.) alone causes modest specific lysis of the target peptide (∼25%). However, treatment with a combination of CL097 and CD40 agonist (10 mg/kg, i.p.) results in an increase of approximately twofold in the specific lysis of the IGRP-peptide-coated targets compared with CL097 treatment alone [3].

Innatura has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

242.28

Molecular Formula

C13H14N4O

Purity

≥98% (HPLC)

Appearance

White to very dark brown powder

Shipping

Room temperature in the continental US; may vary elsewhere.

Storage

2 - 8°C

References

[1]. Cindy Patinote, et al. Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes. Eur J Med Chem. 2020 May 1;193:112238.

[2]. Karama Makni-Maalej, et al. The TLR7/8 agonist CL097 primes N-formyl-methionyl-leucyl-phenylalanine-stimulated NADPH oxidase activation in human neutrophils: critical role of p47phox phosphorylation and the proline isomerase Pin1. J Immunol. 2012 Nov 1;189(9):4657-65.

[3]. A S Lee, et al. Toll-like receptor 7 stimulation promotes autoimmune diabetes in the NOD mouse. Diabetologia. 2011 Jun;54(6):1407-16.

[4] Zhikuan Zhang et al. Cell reports, 25(12), 3371-3381 (2018-12-20), Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands. Toll-like receptor 7 (TLR7) is an innate immune receptor for single-stranded RNA (ssRNA) and has an important role in infectious diseases. We previously reported that TLR7 shows synergistic activation in response to two ligands, guanosine, and ssRNA. However, the specific ssRNA

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