1. Immunology/Inflammation Membrane Transporter/Ion Channel PI3K/Akt/mTOR
  2. mTOR NOD-like Receptor (NLR) Oligopeptide Cotransporter
  3. AJ2-30

AJ2-30 是一种 SLCl5A4 抑制剂。AJ2-30 可抑制内溶酶体 TLR7-9 介导的 mTOR 激活。AJ2-30 可阻断内源性 NOD 信号传导。AJ2-30 可用于炎症研究。

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AJ2-30 Chemical Structure

AJ2-30 Chemical Structure

CAS No. : 2700322-79-6

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

AJ2-30 是一种 SLCl5A4 抑制剂。AJ2-30 可抑制内溶酶体 TLR7-9 介导的 mTOR 激活。AJ2-30 可阻断内源性 NOD 信号传导。AJ2-30 可用于炎症研究[1][2]

In Vitro

AJ2-30 (5 μM, 24 h) inhibits TLR7/8-induced production of TNFα in human monocytes[2].
AJ2-30 (5 μM, 24 h) inhibits TLR7, TLR7/8, and TLR9-induced IFN-α production in human plasmacytoid dendritic cells (pDCs)[2].
AJ2-30 (5 μM) inhibits bacterial dipeptides MDP and TriDAP-mediated NOD1 and NOD2 signaling in primary human macrophages[2].

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

Western Blot Analysis[2]

Cell Line: human B cells
Concentration: 2, 5, 10 μM
Incubation Time: 4 h
Result: Did not block activation of the mTOR pathway upon stimulation with the TLR2 agonist Pam3CSK4.
Reduced the activation of the mTOR pathway in human B cells stimulated with TLR7/8 or TLR9 agonists.
In Vivo

Did not block activation of the mTOR pathway upon stimulation with the TLR2 agonist Pam3CSK4.
Reduced the activation of the mTOR pathway in human B cells stimulated with TLR7/8 or TLR9 agonists.

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

Animal Model: C57BL/6J mice (8-12-week-old) challenged with TLR9 ligand CpG-A complexed with DOTAP[2]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection, prior to CpG-A
Result: Significantly reduced the levels of IFN-α, IFN-β, and IFN-γ in the serum 6 h after CpG-A/DOTAP administration.
Inhibited the phosphorylation of mTOR and 4E-BP1 in splenic pDCs 2 h after CpG-A/DOTAP administration.
Molecular Weight

354.45

Formula

C23H22N4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCN1C2=C(C=CC=C2)C3=CC(CNC4=NC5=C(N4C)C=CC=C5)=CC=C31

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 : 50 mg/mL (141.06 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 2.8213 mL 14.1064 mL 28.2127 mL
5 mM 0.5643 mL 2.8213 mL 5.6425 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.

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

    Solubility: ≥ 5 mg/mL (14.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (14.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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: 99.92%

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, 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8213 mL 14.1064 mL 28.2127 mL 70.5318 mL
5 mM 0.5643 mL 2.8213 mL 5.6425 mL 14.1064 mL
10 mM 0.2821 mL 1.4106 mL 2.8213 mL 7.0532 mL
15 mM 0.1881 mL 0.9404 mL 1.8808 mL 4.7021 mL
20 mM 0.1411 mL 0.7053 mL 1.4106 mL 3.5266 mL
25 mM 0.1129 mL 0.5643 mL 1.1285 mL 2.8213 mL
30 mM 0.0940 mL 0.4702 mL 0.9404 mL 2.3511 mL
40 mM 0.0705 mL 0.3527 mL 0.7053 mL 1.7633 mL
50 mM 0.0564 mL 0.2821 mL 0.5643 mL 1.4106 mL
60 mM 0.0470 mL 0.2351 mL 0.4702 mL 1.1755 mL
80 mM 0.0353 mL 0.1763 mL 0.3527 mL 0.8816 mL
100 mM 0.0282 mL 0.1411 mL 0.2821 mL 0.7053 mL
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  • 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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