Gardiquimod
Based on 2 publication(s) in Google Scholar
Gardiquimod is an imidazoline TLR7/8 agonist. Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 at concentrations below 10 μM.
For research use only. We do not sell to patients.
- Purity : 99.78%
- CAS No.: 1020412-43-4
- Formula: C17H23N5O
- Molecular Weight:313.40
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Gardiquimod
More
Biological Activity
Description
IC50 & Target
[1]|
TLR7 |
TLR8 |
HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HEK293 | EC50 |
2 μM
Compound: 2
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Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene assay
Agonist activity at human TLR7 expressed in NF-kappaB-stimulated HEK293 cells assessed as induction of secreted alkaline phosphatase expression by reporter gene assay
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[PMID: 20481492] |
In Vitro
Gardiquimod (6-60 μM ) significantly inhibits cDNA synthesis by HIV-1 reverse transcriptase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic nude mice (Balb-nu/nu, 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2]
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Dosage:1 mg/kg per mouse
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Administration:i.p.; daily for 7 days
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Result:Significantly suppressed the growth of human HepG2 liver carcinoma xenografts.
Chemical Information
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CAS No. 1020412-43-4
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Appearance Solid
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Molecular Weight 313.40
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Formula C17H23N5O
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Color White to off-white
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SMILES
OC(C)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (319.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.98 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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PBMC Thawing for Immune Assays
PBMC thawing for immune assays recovers viable cryopreserved peripheral blood mononuclear cells for downstream functional or phenotypic readouts, including ELISPOT, intracellular cytokine staining, proliferation assays, and flow-cytometric immunophenotyping. Cryopreserved PBMCs can support immune monitoring because antigen-specific T-cell function and major CD4/CD8 phenotypes may be retained after optimized freezing and thawing, although some lymphocyte subsets and activation or memory markers can be altered by cryopreservation. The technical objective is rapid warming of the frozen vial followed by controlled dilution and removal of DMSO-containing cryomedium, because thawing and wash conditions measurably affect viable PBMC recovery and downstream assay performance. Viability alone is insufficient for protocol evaluation because high viability may occur with low live-cell recovery, so both viable percentage and absolute live-cell recovery should be measured after thawing.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Buitendijk M, et 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. [Content Brief]
[2]. Zhou Z, et al. TLR7/8 agonists promote NK-DC cross-talk to enhance NK cell anti-tumor effects in hepatocellular carcinoma. Cancer Lett. 2015 Dec 28;369(2):298-306. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.1908 mL | 15.9541 mL | 31.9081 mL | 79.7703 mL |
| 5 mM | 0.6382 mL | 3.1908 mL | 6.3816 mL | 15.9541 mL | |
| 10 mM | 0.3191 mL | 1.5954 mL | 3.1908 mL | 7.9770 mL | |
| 15 mM | 0.2127 mL | 1.0636 mL | 2.1272 mL | 5.3180 mL | |
| 20 mM | 0.1595 mL | 0.7977 mL | 1.5954 mL | 3.9885 mL | |
| 25 mM | 0.1276 mL | 0.6382 mL | 1.2763 mL | 3.1908 mL | |
| 30 mM | 0.1064 mL | 0.5318 mL | 1.0636 mL | 2.6590 mL | |
| 40 mM | 0.0798 mL | 0.3989 mL | 0.7977 mL | 1.9943 mL | |
| 50 mM | 0.0638 mL | 0.3191 mL | 0.6382 mL | 1.5954 mL | |
| 60 mM | 0.0532 mL | 0.2659 mL | 0.5318 mL | 1.3295 mL | |
| 80 mM | 0.0399 mL | 0.1994 mL | 0.3989 mL | 0.9971 mL | |
| 100 mM | 0.0319 mL | 0.1595 mL | 0.3191 mL | 0.7977 mL |
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