Gardiquimod diTFA

Name: Gardiquimod diTFA
Brand: MedChemExpress
SKU: HY-103697A
Rating: 4.5 (1 reviews)

Cat. No.: HY-103697A Purity: ≥99.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1159840-61-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 88	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 88	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
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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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Gardiquimod diTFA:

Gardiquimod Get quote

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View All Toll-like Receptor (TLR) Isoform Specific Products:

View All Isoforms

TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

View All HIV Isoform Specific Products:

View All Isoforms

HIV HIV-1 HIV-2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

TLR7

TLR8

HIV-1

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.65 μg/mL Compound: 9	Agonist activity at TLR7 expressed in HEK293 cells assessed as increase in NF-kappaB activation by SEAP assay Agonist activity at TLR7 expressed in HEK293 cells assessed as increase in NF-kappaB activation by SEAP assay	[PMID: 19285861]

In Vitro

Gardiquimod diTFA (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.

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

541.44

Formula

C₂₁H₂₅F₆N₅O₅

CAS No.

1159840-61-5

Appearance

Solid

Color

White to off-white

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (92.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 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

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.
Protocol 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

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (92.35 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥99.0%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (256 KB) HNMR (229 KB)

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]. 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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.8469 mL	9.2346 mL	18.4693 mL	46.1732 mL
	5 mM	0.3694 mL	1.8469 mL	3.6939 mL	9.2346 mL
	10 mM	0.1847 mL	0.9235 mL	1.8469 mL	4.6173 mL
	15 mM	0.1231 mL	0.6156 mL	1.2313 mL	3.0782 mL
	20 mM	0.0923 mL	0.4617 mL	0.9235 mL	2.3087 mL
	25 mM	0.0739 mL	0.3694 mL	0.7388 mL	1.8469 mL
	30 mM	0.0616 mL	0.3078 mL	0.6156 mL	1.5391 mL
	40 mM	0.0462 mL	0.2309 mL	0.4617 mL	1.1543 mL
DMSO	50 mM	0.0369 mL	0.1847 mL	0.3694 mL	0.9235 mL
	60 mM	0.0308 mL	0.1539 mL	0.3078 mL	0.7696 mL
	80 mM	0.0231 mL	0.1154 mL	0.2309 mL	0.5772 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.