TLR9 antagonist 1 diformate

Name: TLR9 antagonist 1 diformate
Brand: MedChemExpress
SKU: HY-178037A
Rating: 4.5 (1 reviews)

Cat. No.: HY-178037A: Data Sheet
SDS
Handling Instructions
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TLR9 antagonist 1 diformate is a selective hTLR9 antagonist with an IC₅₀ of 0.1 nM against hTLR9. TLR9 antagonist 1 diformate exhibits favorable pharmacokinetic and pharmacodynamic properties. TLR9 antagonist 1 diformate can be used in the research of systemic lupus erythematosus.

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

TLR9 antagonist 1 diformate Chemical Structure

Size	Stock	Quantity
Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Liquid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of TLR9 antagonist 1 diformate:

TLR9 antagonist 1 Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

In Vitro

TLR9 antagonist 1 (compound 38) diformate inhibits TLR9 activity in human peripheral blood mononuclear cells with an IC₅₀ of 4 nM^[1].
TLR9 antagonist 1 diformate exerts no significant inhibitory effect on human TLR2, TLR4 or TLR5, and exhibits a selectivity of >10000-fold for these receptors over human TLR9^[1].

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

In Vivo

TLR9 antagonist 1 (1-10 mg/kg; i.p.; single dose) diformate significantly reduces the levels of proinflammatory cytokines induced by TLR9 agonists in C57BL/6J mice^[1].

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

Animal Model:	C57BL/6J mice treated ODN 1668 (HY-150726)^[1]
Dosage:	1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:	i.p.; single dose
Result:	Significantly reduced serum TNF-α levels in ODN1668-challenged mice at both 3 and 6 hours post-treatment. Potently inhibited ODN1826-induced IL-6 secretion.

Molecular Weight

547.65

Formula

C₃₀H₃₇N₅O₅

Appearance

Liquid

SMILES

N#CC1=C2N=CC=CC2=C(N3C(CN(CCCCNCC4=CC=CC=C4OC)C5)C5CC3)C=C1.OC=O.OC=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-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 (182.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8260 mL	9.1299 mL	18.2598 mL
5 mM	0.3652 mL	1.8260 mL	3.6520 mL
10 mM	0.1826 mL	0.9130 mL	1.8260 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.

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 (4.56 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 (4.56 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 (4.56 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.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Data Sheet (274 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[1]. Song X, et al. Discovery of Potent and Selective Quinoline-Based Toll-like Receptor 9 Antagonists. ACS Med Chem Lett. 2025 Aug 26;16(9):1747-1755. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8260 mL	9.1299 mL	18.2598 mL	45.6496 mL
	5 mM	0.3652 mL	1.8260 mL	3.6520 mL	9.1299 mL
	10 mM	0.1826 mL	0.9130 mL	1.8260 mL	4.5650 mL
	15 mM	0.1217 mL	0.6087 mL	1.2173 mL	3.0433 mL
	20 mM	0.0913 mL	0.4565 mL	0.9130 mL	2.2825 mL
	25 mM	0.0730 mL	0.3652 mL	0.7304 mL	1.8260 mL
	30 mM	0.0609 mL	0.3043 mL	0.6087 mL	1.5217 mL
	40 mM	0.0456 mL	0.2282 mL	0.4565 mL	1.1412 mL
	50 mM	0.0365 mL	0.1826 mL	0.3652 mL	0.9130 mL
	60 mM	0.0304 mL	0.1522 mL	0.3043 mL	0.7608 mL
	80 mM	0.0228 mL	0.1141 mL	0.2282 mL	0.5706 mL
	100 mM	0.0183 mL	0.0913 mL	0.1826 mL	0.4565 mL