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

Gardiquimod diTFA 

Cat. No.: HY-103697A Purity: >99.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Gardiquimod diTFA Chemical Structure

Gardiquimod diTFA Chemical Structure

CAS No. : 1159840-61-5

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
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10 mg USD 80 In-stock
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25 mg USD 180 In-stock
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50 mg USD 280 In-stock
Estimated Time of Arrival: December 31
100 mg USD 480 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target[1]

TLR7

 

TLR8

 

HIV-1

 

In Vitro

Gardiquimod diTFA (6-60 μM ) significantly inhibits cDNA synthesis by HIV-1 reverse transcriptase[1].

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].

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

541.44

Formula

C₂₁H₂₅F₆N₅O₅

CAS No.

1159840-61-5

SMILES

OC(C)(C)CN1C(CNCC)=NC2=C1C3=CC=CC=C3N=C2N.FC(C(O)=O)(F)F.FC(C(O)=O)(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (184.69 mM; Need ultrasonic)

H2O : 25 mg/mL (46.17 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8469 mL 9.2346 mL 18.4693 mL
5 mM 0.3694 mL 1.8469 mL 3.6939 mL
10 mM 0.1847 mL 0.9235 mL 1.8469 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Gardiquimod diTFAToll-like Receptor (TLR)HIVHuman immunodeficiency virusHIV-1macrophagesperipheralbloodmononuclearcellsPBMCsHepG2livercarcinomaInhibitorinhibitorinhibit

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Gardiquimod diTFA
Cat. No.:
HY-103697A
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