| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Gardiquimod targets Toll-like receptor 7 (TLR7), a pattern recognition receptor that plays a critical role in innate immune responses. TLR7 recognizes single-stranded RNA and triggers signaling pathways that lead to the production of pro-inflammatory cytokines and type I interferons. Gardiquimod is a potent and specific agonist of TLR7 at concentrations below 10 μM, while at higher concentrations it may also activate TLR8. The compound also inhibits HIV-1 reverse transcriptase, representing a secondary target.
|
|---|---|
| ln Vitro |
HIV-1 reverse transcriptase's ability to synthesize cDNA is markedly inhibited by gardiquimod (6–60 μM) [1].
Gardiquimod inhibits HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). It induces the activation of NF-κB in HEK 293 cells expressing TLR7. The compound induces pro-inflammatory cytokine production in thymocytes. At concentrations below 10 μM, gardiquimod specifically activates TLR7, while at higher concentrations it may activate both TLR7 and TLR8. Its antiproliferative effects have been observed in various cell types. |
| ln Vivo |
Dendritic cells (DC) and gadiquimod (1 mg/kg per mouse; intraperitoneal injection; every day for 7 days) together amplify the natural killer (NK) impact against tumors [2].
Gardiquimod has been studied for its immunomodulatory effects in vivo, particularly in the context of vaccine adjuvant development and cancer immunotherapy. As a TLR7 agonist, it stimulates innate immune responses that can enhance antitumor immunity. The compound's ability to induce pro-inflammatory cytokine production contributes to its immunomodulatory effects. Its potential as a therapeutic agent for viral infections and cancer is being investigated. |
| Enzyme Assay |
In vitro receptor binding assays for gardiquimod involve measuring its binding affinity to TLR7 using cell-based reporter systems. HEK 293 cells expressing TLR7 are treated with the compound, and NF-κB activation is measured using luciferase reporter assays. TLR7 selectivity is assessed by comparing activity in cells expressing TLR7 versus TLR8. HIV-1 reverse transcriptase inhibition is measured using purified enzyme preparations and appropriate substrates. These assays establish the compound's potency and selectivity as a TLR7 agonist.
|
| Cell Assay |
In vitro cell-based assays for gardiquimod involve treating immune cells such as macrophages, PBMCs, or thymocytes with varying concentrations of the compound. Cytokine production (e.g., IFN-α, IL-6, TNF-α) is measured by ELISA. HIV-1 infection inhibition is assessed by measuring viral replication in infected macrophages and PBMCs. NF-κB activation is measured using reporter gene assays in TLR7-expressing cells. Cell proliferation is assessed using standard colorimetric assays. These assays characterize the compound's immunomodulatory and antiviral activities.
|
| Animal Protocol |
Animal/Disease Models: Male athymic nude mice (Balb-nu/nu, 5 weeks old) (carrying human HepG2 liver cancer xenografts) [2]
Doses: 1 mg/kg per mouse Doses: intraperitoneal (ip) injection; one time/day , lasting 7 days. Experimental Results: Dramatically inhibited the growth of human HepG2 liver cancer xenografts. In vivo animal experiments for gardiquimod have been conducted in models of cancer and infectious diseases. The compound is typically administered orally or via injection. As a TLR7 agonist, it stimulates innate immune responses and enhances antitumor immunity. Vaccine adjuvant studies evaluate its ability to enhance antigen-specific immune responses. Efficacy endpoints include tumor growth inhibition, cytokine production, and immune cell activation. Specific dosing regimens and detailed efficacy data are available in the scientific literature. |
| ADME/Pharmacokinetics |
Gardiquimod has a molecular weight of 313.4 and is an imidazoquinoline compound. It is a small-molecule TLR7 agonist with good cell permeability. The compound is typically dissolved in DMSO for in vitro studies and can be formulated for in vivo administration. Its pharmacokinetic properties, including absorption, distribution, metabolism, and elimination, have been characterized in preclinical studies. The compound's stability under recommended storage conditions supports its use in research applications.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for gardiquimod is not extensively reported. As a TLR7 agonist, its immunostimulatory activity may lead to cytokine-related side effects at high doses. The compound's antiproliferative effects suggest potential for selective toxicity. Preclinical toxicology studies have been conducted to establish the safety profile. Standard safety precautions should be taken when handling the compound in research settings.
|
| References |
|
| Additional Infomation |
Gardiquimod is a synthetic imidazoquinoline and a potent, selective TLR7 agonist with antitumor and immunomodulatory effects. It inhibits HIV-1 infection of macrophages and PBMCs and induces pro-inflammatory cytokine production. At concentrations below 10 μM, gardiquimod specifically activates TLR7. The compound has applications in oncology, virology, and vaccine adjuvant development. It is also known as a TLR7/8 agonist.
|
| Molecular Formula |
C17H23N5O
|
|---|---|
| Molecular Weight |
313.3974
|
| Exact Mass |
313.19
|
| CAS # |
1020412-43-4
|
| Related CAS # |
Gardiquimod diTFA;1159840-61-5
|
| PubChem CID |
44592366
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.019
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
23
|
| Complexity |
404
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
0
|
| Synonyms |
Gardiquimod TFA salt Gardiquimod
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMF :≥ 20 mg/mL (~63.82 mM)
DMSO : ≥ 20 mg/mL (~63.82 mM) Ethanol :≥ 12 mg/mL (~38.29 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA