1. Immunology/Inflammation
  2. Toll-like Receptor (TLR)
  3. IAXO-102

IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.

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

IAXO-102 Chemical Structure

IAXO-102 Chemical Structure

CAS No. : 1115270-63-7

Size Price Stock Quantity
Solution
10 mM * 1 mL in Ethanol USD 413 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 320 In-stock
10 mg USD 510 In-stock
50 mg USD 1500 In-stock
100 mg USD 2400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 4 publication(s) in Google Scholar

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  • Purity & Documentation

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Description

IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development[1].

IC50 & Target[1]

TLR4

 

In Vitro

IAXO-102 (1-10 µM, for 2 hours) inhibits MAPK and p65 NF-κB phosphorylation in human umbilical vein endothelial (HUVEC) cells[1].
IAXO-102 (10 µM, for 17 hours) suppresses LPS induced proinflammatory proteins MCP-1 and IL-8 production in HUVEC[1].

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

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial (HUVEC) cells
Concentration: 1-10 µM
Incubation Time: Pretreatment for 1 hour and then exposed to LPS (100 ng/mL) for additional 1 hour
Result: Significantly inhibited LPS-stimulated MAPK/p65nF-ΚB phosphorylation.
In Vivo

IAXO-102 (3 mg/kg/day, s.c. for 28 days) significantly retards Angiotensin II induced increase in aortic diameter in mice[1].

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

Animal Model: Six-monthold ApoE−/−/C57Bl6[1]
Dosage: 3 mg/kg/day
Administration: S.C. for 28 days
Result: Significantly retarded Angiotensin II-induced increase in aortic diameter.
Molecular Weight

585.94

Formula

C35H71NO5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCCCCCCCCCCCCO[C@@H]1[C@H]([C@@H]([C@@H](CN)O[C@@H]1OC)O)OCCCCCCCCCCCCCC

Shipping

Room temperature in continental US; may vary elsewhere.

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

Ethanol : 50 mg/mL (85.33 mM; Need ultrasonic)

DMSO : 3.33 mg/mL (5.68 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 1.7067 mL 8.5333 mL 17.0666 mL
5 mM 0.3413 mL 1.7067 mL 3.4133 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.83 mg/mL (1.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (8.3 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% EtOH    90% Corn Oil

    Solubility: ≥ 0.83 mg/mL (1.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.83 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 EtOH stock solution (8.3 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)

g

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
References

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, 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 / Ethanol 1 mM 1.7067 mL 8.5333 mL 17.0666 mL 42.6665 mL
5 mM 0.3413 mL 1.7067 mL 3.4133 mL 8.5333 mL
Ethanol 10 mM 0.1707 mL 0.8533 mL 1.7067 mL 4.2666 mL
15 mM 0.1138 mL 0.5689 mL 1.1378 mL 2.8444 mL
20 mM 0.0853 mL 0.4267 mL 0.8533 mL 2.1333 mL
25 mM 0.0683 mL 0.3413 mL 0.6827 mL 1.7067 mL
30 mM 0.0569 mL 0.2844 mL 0.5689 mL 1.4222 mL
40 mM 0.0427 mL 0.2133 mL 0.4267 mL 1.0667 mL
50 mM 0.0341 mL 0.1707 mL 0.3413 mL 0.8533 mL
60 mM 0.0284 mL 0.1422 mL 0.2844 mL 0.7111 mL
80 mM 0.0213 mL 0.1067 mL 0.2133 mL 0.5333 mL
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IAXO-102 Related Classifications

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.

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IAXO-102
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HY-125171
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