TLR7/8/9-IN-1

Name: TLR7/8/9-IN-1
Brand: MedChemExpress
SKU: HY-131952
Rating: 5.0 (2 reviews)

Cat. No.: HY-131952 Purity: 98.51%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC₅₀ = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).

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

CAS No. : 2180127-82-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + 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
Solid
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	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE TLR7/8/9-IN-1

Cell Imaging/Staining

: TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Adv Biol (Weinh). 2025 Jun 4:e00761. [Abstract]; Macrophages were pretreated with inhibitors of TLR2 (MMG-11; HY‐112146), TLR4 (Resatorvid; HY‐11109), TLR9 (TLR7/8/9-IN-1; HY-131952) and RAGE (RAGE antagonist peptide; HY‐P2268) prior to coculture with pyroptotic‐CM, and the p‐p38 and p‐p65 levels in macrophages were measured by western blotting.

: TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]; Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the p-p38 level in neutrophils was measured by western blotting.

: TLR7/8/9-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2023 May 1;21(1):86. [Abstract]; Neutrophils isolated from healthy individuals were pretreated with inhibitors of TLR2 (HY-112146; MMG-11), TLR4 (HY-107575; TLR4-IN-C34 ), TLR9 (HY-131952; TLR7/8/9-IN-1) and RAGE (HY-P2268; RAGE antagonist peptide) for 1 h prior to coculture with hypoxic-CM from GC cells, and the NET formation was detected with MPO and citH3 staining. Magnification: 20 × . Scale bars: 50 μm. All values are the means ± SDs. ns = not significant, **P < 0.01

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Biological Activity
Purity & Documentation
References
Customer Review

Description

TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC₅₀ = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 50000 nM Compound: 7f	Agonist activity at human TLR7 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay Agonist activity at human TLR7 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay	[PMID: 32944143]
HEK293	IC₅₀	> 50000 nM Compound: 7f	Agonist activity at human TLR8 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay Agonist activity at human TLR8 overexpressed in HEK293 cells assessed as NFkappaB expression by reporter gene assay	[PMID: 32944143]
PBMC	IC₅₀	4.8 nM Compound: 7f	Antagonist activity at TLR7 (unknown origin) in PBMC cells assessed as reduction of IL-6 production Antagonist activity at TLR7 (unknown origin) in PBMC cells assessed as reduction of IL-6 production	[PMID: 32944143]
PBMC	IC₅₀	510 nM Compound: 7f	Antagonist activity at TLR9 (unknown origin) in PBMC cells assessed as reduction of IL-6 production Antagonist activity at TLR9 (unknown origin) in PBMC cells assessed as reduction of IL-6 production	[PMID: 32944143]

Molecular Weight

435.60

Formula

C₂₇H₃₇N₃O₂

CAS No.

2180127-82-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

CNCCN1CCC(C2=CC3=C(NC(C4=CC=C(OC)C(OC)=C4)=C3C(C)C)C=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 83.33 mg/mL (191.30 mM; ultrasonic and warming and heat to 60°C; 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	2.2957 mL	11.4784 mL	22.9568 mL
5 mM	0.4591 mL	2.2957 mL	4.5914 mL
10 mM	0.2296 mL	1.1478 mL	2.2957 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 (protect from light). 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: ≥ 2.08 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.78 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 98.51%

Select Batch:

Data Sheet (270 KB) SDS (252 KB)

COA (246 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Mussari CP, et al. Discovery of Potent and Orally Bioavailable Small Molecule Antagonists of Toll-like Receptors 7/8/9 (TLR7/8/9). ACS Med Chem Lett. 2020 Jul 29;11(9):1751-1758. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2957 mL	11.4784 mL	22.9568 mL	57.3921 mL
	5 mM	0.4591 mL	2.2957 mL	4.5914 mL	11.4784 mL
	10 mM	0.2296 mL	1.1478 mL	2.2957 mL	5.7392 mL
	15 mM	0.1530 mL	0.7652 mL	1.5305 mL	3.8261 mL
	20 mM	0.1148 mL	0.5739 mL	1.1478 mL	2.8696 mL
	25 mM	0.0918 mL	0.4591 mL	0.9183 mL	2.2957 mL
	30 mM	0.0765 mL	0.3826 mL	0.7652 mL	1.9131 mL
	40 mM	0.0574 mL	0.2870 mL	0.5739 mL	1.4348 mL
	50 mM	0.0459 mL	0.2296 mL	0.4591 mL	1.1478 mL
	60 mM	0.0383 mL	0.1913 mL	0.3826 mL	0.9565 mL
	80 mM	0.0287 mL	0.1435 mL	0.2870 mL	0.7174 mL
	100 mM	0.0230 mL	0.1148 mL	0.2296 mL	0.5739 mL

TLR7/8/9-IN-1 Related Classifications

Inflammation/Immunology

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:

TLR7/8/9-IN-12180127-82-4Toll-like Receptor (TLR)Inhibitorinhibitorinhibit

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TLR7/8/9-IN-1

Customer Review

TLR7/8/9-IN-1 Related Antibodies

2 Publications Citing Use of MCE TLR7/8/9-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

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

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

TLR7/8/9-IN-1 Related Classifications

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