Gardiquimod |
Catalog No.GC14864 |
agonist of human toll-like receptor 7 (TLR7)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1020412-43-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Gardiquimod is an agonist of human toll-like receptor 7 (TLR7) [1][2].
Toll-like receptors (TLRs) are a family of highly conserved pattern recognition receptors involved in innate immune responses to pathogen infection. TLR7 is highly expressed by plasmacytoid dendritic cells, and is also found on other leukocyte subpopulations. TLR7 and TLR8 recognize single-stranded RNA from viruses [4].
Gardiquimod is an agonist of human toll-like receptor 7 (TLR7), but not human TLR8, although it activates both porcine TLR7 and TLR8. In transfected 293T cells, Gardiquimod preferentially activated porcine TLR8 (pTLR8) [1]. Gardiquimod is a member of imidazoquinoline family. When codelivered intranasally with plant-derived Norwalk virus virus-like particles (NV VLPs), gardiquimod (GARD) induced NV VLP-specific serum IgG and IgG isotype responses and mucosal IgA responses in the gastrointestinal, respiratory, and reproductive tracts [3]. In macrophages and activated peripheral blood mononuclear cells (PBMCs) infected with X4, R5 or dual-tropic (R5/X4) strains of HIV-1, Gardiquimod inhibited HIV-1 reverse transcriptase and significantly reduced infection. Gardiquimod also induced interferon-alpha (IFN-a) transcription and sustained IFN-a protein secretion [4]. In BxPC-3 cells, Gardiquimod inhibited cell proliferation and migration, and induced apoptosis [5].
In C57BL/6 mice, Gardiquimod enhanced the ability of Treg cell to suppress the proliferation of Tresp cells. The CD4+CD25+Treg cells from mice that had received gardiquimod exhibited an increased inhibitory effect on anti-CD3/anti-CD28 mAb-coated bead-stimulated Tresp cells [2].
References:
[1]. Zhu J, Lai K, Brownile R, et al. Porcine TLR8 and TLR7 are both activated by a selective TLR7 ligand, imiquimod. Mol Immunol. 2008 Jun;45(11):3238-43.
[2]. Forward NA1, Furlong SJ, Yang Y, et al. Signaling through TLR7 enhances the immunosuppressive activity of murine CD4+CD25+ T regulatory cells. J Leukoc Biol. 2010 Jan;87(1):117-25.
[3]. Velasquez LS, Hjelm BE, Arntzen CJ, et al. An intranasally delivered Toll-like receptor 7 agonist elicits robust systemic and mucosal responses to Norwalk virus-like particles. Clin Vaccine Immunol. 2010 Dec;17(12):1850-8.
[4]. Buitendijk M, Eszterhas SK, Howell AL. Gardiquimod: a Toll-like receptor-7 agonist that inhibits HIV type 1 infection of human macrophages and activated T cells. AIDS Res Hum Retroviruses. 2013 Jun;29(6):907-18.
[5]. Zou BB, Wang F, Li L, et al. Activation of Toll-like receptor 7 inhibits the proliferation and migration, and induces the apoptosis of pancreatic cancer cells. Mol Med Rep. 2015 Oct;12(4):6079-85.
Cas No. | 1020412-43-4 | SDF | |
Chemical Name | 4-amino-2-[(ethylamino)methyl]-α,α-dimethyl-1H-imidazo[4,5-c]quinoline-1-ethanol | ||
Canonical SMILES | NC1=NC2=C(C3=C1N=C(CNCC)N3CC(C)(O)C)C=CC=C2 | ||
Formula | C17H23N5O | M.Wt | 313.4 |
Solubility | ≤12mg/ml in ethanol;20mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL |
5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL |
10 mM | 0.3191 mL | 1.5954 mL | 3.1908 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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