Art. -Nr.: HY-128598

MD2-TLR4-IN-1

1 Cited Publications

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MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex antagonist. MD2-TLR4-IN-1 inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced expression of TNF-α and IL-6 in macrophages with IC₅₀ values of 0.89 μM and 0.53 μM, respectively. MD2-TLR4-IN-1 can be used for the study of acute lung injury (ALI).

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Reinheit: 98.16%
CAS. Nr.: 2249801-12-3
Formel: C₂₂H₁₄Cl₂N₄O
Molecular Weight:421.28

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

MD2-TLR4-IN-1 Chemical Structure

CAS. Nr.: 2249801-12-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

TLR4

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

In Vitro

MD2-TLR4-IN-1 (compound 22m) exerts its anti-inflammatory activity by inhibiting NF-κB in RAW264.7 macrophages^[1].
MD2-TLR4-IN-1 is directly bound to the MD2-TLR4 complex and disrupted MD2-TLR4 activation^[1].
MD2-TLR4-IN-1 suppresses the NF-κB p65 subunit nuclear levels in LPS-induced macrophages^[1].
MD2-TLR4-IN-1 binds to recombinant MD2 and TLR4 proteins with K_d values of 185 and 146 μM, respectively, while it does not interact with the intracellular adaptor protein MyD88^[1].
MD2-TLR4-IN-1 significantly inhibits dimerization of the MD2-TLR4 complex in LPS-activated mouse primary macrophages (MPMs)^[1].

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

In Vivo

MD2-TLR4-IN-1 (compound 22m) (5-10 mg/kg; tail vein injection; once; 15 min before LPS injection) significantly inhibits macrophage infiltration and ameliorated histopathological changes in lung tissues of LPS-challenged mice^[1].

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

Animal Model:

Male C57BL/6 mice (18-22 g) injectied intraperitoneally with LPS (20 mg/kg)^[1].
Dosage:

5 mg/kg, 10 mg/kg
Administration:

Tail vein injection; once; 15 min before LPS injection
Result:

Effectively reduced airspace inflammation and amended the tissue structure of pulmonary lobules.
Significantly decreases LPS-induced myeloperoxidase (MPO) activity. Reduced LPS-induced serum TNF-α levels.
Decreased the mRNA levels of TNF-α, IL-6, IL-1β, IL-12, and IL-33 in lung tissues. In addition, COX-2 mRNA levels were also reduced.

Chemical Information

CAS. Nr. 2249801-12-3
Appearance Solid
Molecular Weight 421.28
Formel C₂₂H₁₄Cl₂N₄O
Color White to off-white
SMILES

ClC1=C(C(NC2=CC(C(C3=CC=C(NC=C4)C4=C3)=NN5)=C5C=C2)=O)C(Cl)=CC=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

J Funct Foods

2025 Oct 31;135:107084.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 83.33 mg/mL (197.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3737 mL

11.8686 mL

23.7372 mL

5 mM

0.4747 mL

2.3737 mL

4.7474 mL

10 mM

0.2374 mL

1.1869 mL

2.3737 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (4.94 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Liu Z, et al. Discovery of 3-(Indol-5-yl)-indazole Derivatives as Novel Myeloid Differentiation Protein 2/Toll-like Receptor 4 Antagonists for Treatment of Acute Lung Injury. J Med Chem. 2019 Jun 13;62(11):5453-5469. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3737 mL	11.8686 mL	23.7372 mL	59.3430 mL
	5 mM	0.4747 mL	2.3737 mL	4.7474 mL	11.8686 mL
	10 mM	0.2374 mL	1.1869 mL	2.3737 mL	5.9343 mL
	15 mM	0.1582 mL	0.7912 mL	1.5825 mL	3.9562 mL
	20 mM	0.1187 mL	0.5934 mL	1.1869 mL	2.9671 mL
	25 mM	0.0949 mL	0.4747 mL	0.9495 mL	2.3737 mL
	30 mM	0.0791 mL	0.3956 mL	0.7912 mL	1.9781 mL
	40 mM	0.0593 mL	0.2967 mL	0.5934 mL	1.4836 mL
	50 mM	0.0475 mL	0.2374 mL	0.4747 mL	1.1869 mL
	60 mM	0.0396 mL	0.1978 mL	0.3956 mL	0.9890 mL
	80 mM	0.0297 mL	0.1484 mL	0.2967 mL	0.7418 mL
	100 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5934 mL

Keywords

MD2-TLR4-IN-1

1 Cited Publications

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MD2-TLR4-IN-1

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Publications Citing Use of MedChemExpress (MCE) MD2-TLR4-IN-1

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MD2-TLR4-IN-1 Related Classifications

HY-128598 Related Classifications