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MedChemExpress

HY-139397

TJ-M2010-5

TJ-M2010-5

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].
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

Light yellow to 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)

Preparing
Stock Solutions
ConcentrationSolventMass 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
10 mM 0.2460 mL 1.2299 mL 2.4598 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

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