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Chemical Structure| 1357471-57-8 Chemical Structure| 1357471-57-8

Structure of TJ-M2010-5
CAS No.: 1357471-57-8

Chemical Structure| 1357471-57-8

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TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88, preventing its homodimerization and downstream TLR/MyD88 signaling. It is often used in research on myocardial ischemia/reperfusion injury (MIRI), showing protective effects against myocardial damage.

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Product Details of TJ-M2010-5

CAS No. :1357471-57-8
Formula : C23H26N4OS
M.W : 406.54
SMILES Code : O=C(NC1=NC(C2=CC=CC=C2)=CS1)CCN3CCN(CC4=CC=CC=C4)CC3
MDL No. :MFCD34578278
InChI Key :DTIQJBUDKQVBLT-UHFFFAOYSA-N
Pubchem ID :71542350

Safety of TJ-M2010-5

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of TJ-M2010-5

pyroptosis
TLR

Isoform Comparison

Biological Activity

Description
TJ-M2010-5, a MyD88 inhibitor, interacts with the TIR domain of MyD88 to block its homodimerization and disrupt the TLR/MyD88 signaling pathway [1][2].

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary microglia 30 µM 24 hours TJ-M2010-5 inhibited CORT-induced microglial activation, as indicated by reduced immunofluorescence intensity of CD68 and Iba1. Brain Behav Immun. 2023 Feb;108:204-220
BV2 cells 30 µM 24 hours TJ-M2010-5 inhibited CORT-induced neuroinflammatory activation, as indicated by reduced levels of NF-κB p65 phosphorylation and IL-1β protein. Brain Behav Immun. 2023 Feb;108:204-220
SH-SY5Y cells 0, 1, 5, 10, 20, 30 µM 24 hours Evaluate the effect of TJ-M2010-5 on SH-SY5Y cell viability, results showed TJ-5 did not affect cell viability at concentrations below 20 μM Front Pharmacol. 2022 Dec 15;13:1080438
BV-2 cells 0, 1, 5, 10, 20, 30 µM 24 hours Evaluate the effect of TJ-M2010-5 on BV-2 cell viability, results showed TJ-5 did not affect cell viability at concentrations below 20 μM Front Pharmacol. 2022 Dec 15;13:1080438
RAW 264.7 cells 40 µM 4 hours To evaluate the effect of TJ-M2010-5 on cytokine secretion in RAW 264.7 cells. Results showed that TJ-M2010-5 significantly reduced the secretion of GM-CSF, IFN-γ, IL-1β, IL-6, and TGF-β1. Invest New Drugs. 2022 Jun;40(3):506-518
RAW264.7 cells 10 and 20 µM 6 hours TJ-M2010-5 significantly inhibited LPS-induced inflammation by down-regulating the expression of IL6, IL1β, and TNFα, reversed macrophage M1 polarisation, decreased the M1/M2 ratio, and inhibited NO production. Vet Res. 2025 Feb 4;56(1):28
Bone marrow-derived macrophages (BMDMs) 10 and 30 µM 6 hours LPS stimulation followed by 2 hours ATP stimulation To evaluate the inhibitory effect of TJ-5 on LPS- and ATP-induced pyroptosis in BMDMs. Results showed that TJ-5 effectively inhibited GSDMD cleavage and cell death. Transplantation. 2023 Feb 1;107(2):392-404

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Chronic social defeat stress (CSDS) model Intraperitoneal injection 2.5 mg/kg Twice daily for 2 days TJ-M2010-5 alleviated CSDS-induced depressive-like behaviors, as evidenced by increased social interaction time and sucrose preference, and reduced immobility time in TST and FST. Brain Behav Immun. 2023 Feb;108:204-220
BALB/c mice Early infection model of T. spiralis Intraperitoneal injection 30 mg/kg/day Five successive days TJ-M2010-5 significantly alleviated spleen impairment and reduced inflammation in mice infected with T. spiralis in its early stages by blocking the activation of PI3K/miR-136-5p/AKT3 pathway. Vet Res. 2025 Feb 4;56(1):28
C57BL/6 mice Middle cerebral artery occlusion (MCAO) model Intravenous injection 5, 10, 15 mg/kg Single dose, lasted for 24 hours Evaluate the therapeutic effect of TJ-M2010-5 on cerebral ischemia-reperfusion injury, results showed TJ-5 significantly reduced cerebral infarction volume and neuronal loss Front Pharmacol. 2022 Dec 15;13:1080438
Female BalB/c mice Colitis-associated colorectal cancer (CAC) model Intraperitoneal injection 50 mg/kg Daily for 10 weeks To evaluate the effect of TJ-M2010-5 on MDSC accumulation and function in the CAC model. Results showed that TJ-M2010-5 significantly reduced the accumulation of CD11b+Gr-1+ MDSCs, decreased the secretion of cytokines (GM-CSF, G-CSF, IL-1β, IL-6, and TGF-β) associated with MDSC accumulation, and reduced the expression of molecules (iNOS, Arg-1, and IDO) associated with the suppressive capacity of MDSCs. Invest New Drugs. 2022 Jun;40(3):506-518
BALB/c mice Hepatic ischemia-reperfusion injury (IRI) model Intraperitoneal injection 50 mg/kg 3 consecutive days, once daily To evaluate the protective effect of TJ-5 on hepatic IRI. Results showed that TJ-5 significantly improved liver function and reduced hepatocellular injury and inflammation. Transplantation. 2023 Feb 1;107(2):392-404
C57BL/6J mice DSS-induced acute colitis model Intraperitoneal injection 50 mg/kg Once daily, starting one day before the first DSS administration until the seventh day of DSS challenge. To investigate the impact of MyD88 inhibition on DSS-induced acute colitis. Results showed that although TJ5 significantly reduced NF-κB activation, it did not significantly alleviate the severity of colitis. Precis Clin Med. 2024 Jun 6;7(2):pbae013

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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