Imiquimod VacciGrade™

Imidazoquinoline compound

The imidazoquinoline compound Imiquimod is a guanosine derivative and agonist for TLR7.

This TLR7 agonist, originally developed as type I IFN inducers, is an effective adjuvant by activating dendritic cells (DCs) and B cells to induce cytokines optimal for Th1 cell immunity, and antibody production.

Unlike other commercially available Imiquimod preparations, InvivoGen's Imiquimod VacciGrade™ is controlled for TLR7/8 potency and TLR4/TLR2 contamination.

Imiquimod VacciGrade™ is a high-quality pre-clinical grade.
Imiquimod VacciGrade™​ is for research use only, and not for human or veterinary use.

Specifications

Description: TLR7 agonist VacciGrade™

Polarization of adaptive immune response: Th1 response

Formula: C₁₄H₁₆N₄•HCl

Molecular weight: 276.8 g/mol

Solubility: 1 mg/ml in physiological water

Working concentration: 10 - 100 μg/mouse

Quality control:

• Sterility guaranteed
• The absence of bacterial contamination (lipoproteins & endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells
• Endotoxin level < 5 EU/mg (measurement by kinetic chromogenic LAL assay)

Contents

• 5 mg of sterile lyophilized Imiquimod VacciGrade™
• 10 ml sterile endotoxin-free physiological water (NaCl 0.9%)

Imiquimod VacciGrade™ is shipped at room temperature

Stored at -20°C.

Lyophilized product is stable for 1 year when properly stored.

Upon resuspension, prepare aliquots of Imiquimod VacciGrade™ and store at -20°C for long term storage.

Resuspended product is stable for 6 months when properly stored.

Avoid repeated freeze-thaw cycles.

VacciGrade™

VacciGrade™ is a high-quality pre-clinical grade. VacciGrade™ products are filter-sterilized (0.2 µm) and filled under strict aseptic conditions in a clean room*. The absence of bacterial contamination is assessed by a sterility test using a pharmacopeia-derived assay. The level of bacterial contaminants (endotoxins and lipoproteins) in each lot is verified using a LAL assay and/or a TLR2 and TLR4 reporter assay.
*Except for LPS VacciGrade™, which is prepared in a laminar flow hood dedicated to LPS.

Details

Imiquimod (R837), an imidazoquinoline amine analog to guanosine, is an immune response modifier with potent antiviral and antitumor activities [1].

Imiquimod is approved for the topical treatment of genital warts, basal cell carcinoma, and bladder cancer. Imiquimod exerts its immune-modulating activity by inducing the production of pro-inflammatory cytokines, such as IFN-α and IL-12, leading to the activation of both innate and acquired immunity [2]. This activity of Imiquimod is in part due to its capacity to bind to and stimulate Toll-like receptor (TLR)-7, suggesting a potential role of Imiquimod to act as an adjuvant [3, 4].

Preclinical studies in mice have shown the effectiveness of Imiquimod in inducing immune responses to immunization using various vaccination strategies [5-7]. Imiquimod has been shown to increase both antibody and cell-mediated immune responsiveness induced by a DNA vaccine. In a genetically engineered mouse model, a DNA vaccine encoding HER2/neu adjuvanted with Imiquimod was reported to significantly delay the development of spontaneous mammary tumors [6]. This antitumor effect was accompanied by a significant increase in Ag-specific antibody (Ab) production and in CTL activity, and a switch from IgG1 to IgG2a Ab isotype, suggesting a Th1 polarization of the immune response.

1. Suader DN., 2000. Immunomodulatory and pharmacologic properties of Imiquimod. J Am Acad Dermatol 43: S6−S11.
2. Stanley MA., 2002. Imiquimod and the imidazoquinolines: mechanism of action and therapeutic potential. Clin Dermatol 27:571−577.
3. Hemmi H. et al. 2002. Small anti-viral compounds activate immune cells via the TLR7 MyD88-dependent signaling pathway. Nat Immunol, 3(2):196-200.
4. Schon MP & Schon M., 2004. Immune modulation and apoptosis induction: two sides of the antitumoral activity of Imiquimod. Apoptosis 9: 291−298.
5. Thomsen LL et al.., 2004. Imiquimod and resiquimod in a mouse model: adjuvants for DNA vaccination by particle mediated immunotherapeutic delivery. Vaccine 22: 1799−1809.
6. Smorlesi A. et al.,2005. Imiquimod and S-27609 as adjuvants of DNA vaccination in a transgenic murine model of HER2/neu-positive mammary carcinoma. Gene Ther. 12(17):1324-32.
7.Triozzi PL. et al., 2010. Regulation of the activity of an adeno-associated virus vector cancer vaccine administered with synthetic Toll-like receptor agonists. Vaccine. 28(50):7837-43.