2. Immunology/Inflammation Anti-infection
  3. Toll-like Receptor (TLR) HIV
  4. Gardiquimod

Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10?μM.

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Gardiquimod Chemical Structure

Gardiquimod Chemical Structure

CAS No. : 1020412-43-4

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Based on 1 publication(s) in Google Scholar

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Gardiquimod Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10?μM[1][2].

IC50 & Target[1]

TLR7

 

TLR8

 

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
2 μM
Compound: 2
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
[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.

Gardiquimod Related Antibodies
In Vivo

Dendritic cells (DCs) in combination with Gardiquimod (1 mg/kg per mouse; i.p.; daily for 7 days) improves the anti-tumor effects of NK cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male athymic nude mice (Balb-nu/nu, 5 weeks old) (bearing human HepG2 liver carcinoma xenografts)[2]
Dosage: 1 mg/kg per mouse
Administration: i.p.; daily for 7 days
Result: Significantly suppressed the growth of human HepG2 liver carcinoma xenografts.
Molecular Weight

313.40

Formula

C17H23N5O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(C)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : ≥ 20 mg/mL (63.82 mM)

DMSO : ≥ 20 mg/mL (63.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 12 mg/mL (38.29 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.91%

SDS (393 KB)

COA (253 KB) HNMR (283 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

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
Ethanol / DMF / 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
DMF / DMSO 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
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Gardiquimod Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gardiquimod1020412-43-4Toll-like Receptor (TLR)HIVHuman immunodeficiency virusHIV-1macrophagesperipheralbloodmononuclearcellsPBMCsHepG2livercarcinomaInhibitorinhibitorinhibit

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