2. Immunology/Inflammation
  3. MyD88
  4. TJ-M2010-5

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).

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

TJ-M2010-5 Chemical Structure

TJ-M2010-5 Chemical Structure

CAS No. : 1357471-57-8

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Customer Review

Based on 13 publication(s) in Google Scholar

TJ-M2010-5 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway[1][2]. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI)[2].

Cellular Effect
Cell Line Type Value Description References
Peritoneal macrophage IC50
10.25 μM
Compound: 6; TJ-M2010-5
Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA
Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA
[PMID: 30342423]
Peritoneal macrophage IC50
11.88 μM
Compound: 6; TJ-M2010-5
Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA
Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA
[PMID: 30342423]
In Vitro

TJ-M2010-5 (40 μM) inhibits MyD88 homodimerization in transfected HEK293 cells in a concentration-dependent manner and suppresses MyD88 signaling in LPS (100 ng/mL)-responsive RAW 264.7 cells in vitro[1].
? TJ-M2010-5 (5-30 μM) prevents B cell proliferation and induces B cells apoptosis after stimulation with R848 (500 ng/mL)[3].

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

TJ-M2010-5 Related Antibodies

Cell Viability Assay[3]

Cell Line: Purified B cells
Concentration: 0 μM, 5 μM, 10 μM, 20 μM and 30 μM
Incubation Time: 48 hours
Result: Inhibited the viability of B cells with or without the stimulation of CD40L.
In Vivo

TJ-M2010-5 treatment statistically significantly reduces AOM/DSS-induced colitis and completely prevented CAC development with less related body mass loss, results in 0% mortality of treated mice, decreases cell proliferation, and increased apoptosis in colon tissue in a 10-week CAC mouse model[1].
? TJ-M2010-5 statistically significantly decreases TNF-α, IL-6, G-CSF, MIP-1β, IL-11, IL-17A, IL-22, and IL-23 serum concentrations in mice at both two and seven weeks postinduction, as well as TGF-β1 serum levels at seven weeks postinduction[1].

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

Animal Model: Female BalB/c mice (6–8 weeks old) [1]
Dosage: 50 mg/kg
Administration: Treated i.p. daily beginning two days before the first dextran sodium sulfate (DSS) administration throughout a 10-week observation period.
Result: Significantly prevented inflammation/CAC-related body weight loss and mortality (0% vs 53% in the control group).
Molecular Weight

406.54

Formula

C23H26N4OS
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(NC1=NC(C2=CC=CC=C2)=CS1)CCN3CCN(CC4=CC=CC=C4)CC3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (245.98 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 2.4598 mL 12.2989 mL 24.5978 mL
5 mM 0.4920 mL 2.4598 mL 4.9196 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 (protect from light, stored under nitrogen). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (6.15 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 (6.15 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
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).

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

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: 99.85%

SDS (393 KB)

COA (245 KB) HNMR (254 KB) RP-HPLC (299 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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 (protect from light, stored under nitrogen). 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 2.4598 mL 12.2989 mL 24.5978 mL 61.4946 mL
5 mM 0.4920 mL 2.4598 mL 4.9196 mL 12.2989 mL
10 mM 0.2460 mL 1.2299 mL 2.4598 mL 6.1495 mL
15 mM 0.1640 mL 0.8199 mL 1.6399 mL 4.0996 mL
20 mM 0.1230 mL 0.6149 mL 1.2299 mL 3.0747 mL
25 mM 0.0984 mL 0.4920 mL 0.9839 mL 2.4598 mL
30 mM 0.0820 mL 0.4100 mL 0.8199 mL 2.0498 mL
40 mM 0.0615 mL 0.3075 mL 0.6149 mL 1.5374 mL
50 mM 0.0492 mL 0.2460 mL 0.4920 mL 1.2299 mL
60 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0249 mL
80 mM 0.0307 mL 0.1537 mL 0.3075 mL 0.7687 mL
100 mM 0.0246 mL 0.1230 mL 0.2460 mL 0.6149 mL
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TJ-M2010-5 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.

Keywords:

TJ-M2010-51357471-57-8MyD88MyD88,TLRmyocardialischemiareperfusioninjury MIRIAnoxiareoxygenationmyeloiddifferentiationfactorinjuryremodelingInhibitorinhibitorinhibit

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