| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
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| ln Vitro |
Gardiquimod diTFA (6–60 μM) dramatically reduces HIV-1 reverse transcriptase's ability to synthesize cDNA[1].
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| ln Vivo |
The anti-tumor actions of NK cells are enhanced when Dendritic cells (DCs) and Gardiquimod (1 mg/kg per mouse; ip; daily for 7 days) are combined[2].
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| Animal Protocol |
Animal/Disease Models: Male athymic nude mice (Balb-nu/nu , 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2]
Doses: 1 mg/kg per mouse Route of Administration: ip; daily for 7 days Experimental Results: Dramatically suppressed the growth of human HepG2 liver carcinoma xenografts. |
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| 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.
[2]. Ma F, et al. The TLR7 agonists imiquimod and gardiquimod improve DC-based immunotherapy for melanoma in mice. Cell Mol Immunol. 2010 Sep;7(5):381-8. [3]. 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. |
| Molecular Formula |
C19H24F3N5O3
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| Molecular Weight |
427.43
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| CAS # |
1159840-61-5
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| Related CAS # |
Gardiquimod;1020412-43-4
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| SMILES |
CC(O)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N.O=C(O)C(F)(F)F
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| Chemical Name |
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (92.35 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3396 mL | 11.6978 mL | 23.3956 mL | |
| 5 mM | 0.4679 mL | 2.3396 mL | 4.6791 mL | |
| 10 mM | 0.2340 mL | 1.1698 mL | 2.3396 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Gardiquimod and imiquimod promote proliferation of splenocytes.
Gardiquimod and imiquimod increase the cytotoxicity of splenocytes.Cell Mol Immunol.2010 Sep;7(5):381-8. |
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Gardiquimod and imiquimod enhance the activation of splenocytes.Cell Mol Immunol.2010 Sep;7(5):381-8. |
Gardiquimod and imiquimod promote the expression of costimulatory molecules on macrophages and dendritic cells.
Combination therapy with gardiquimod or imiquimod and DC vaccine inhibits the growth of subcutaneous B16 melanomas.Cell Mol Immunol.2010 Sep;7(5):381-8. |
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