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 inhibited MyD88 homodimerization in transfected HEK293 cells in a concentration-dependent manner and suppressed MyD88 signaling in LPS-responsive RAW 264.7 cells in vitro.
In a 10-week CAC mouse model (n = 30 per group), TJ-M2010-5 treatment statistically significantly reduced AOM/DSS-induced colitis and completely prevented CAC development with less related body mass loss, resulted in 0% mortality of treated mice (compared with 53% mortality of control mice), decreased cell proliferation, and increased apoptosis in colon tissue. TJ-M2010-5 treatment also inhibited production of inflammatory cytokines and chemokines (TNF-α, IL-6,G-CSF, MIP-1β, TGF-β1, IL-11, IL-17A, IL-22 and IL-23) and infiltration of immune cells (macrophages, dendritic cells, neutropihls and CD(+)4 T cells) in colon tissues of mice.
|Cell lines||RAW 264.7 cells|
|Preparation method||RAW 264.7 cells were cultured in RPMI medium 1640. After stimulation with 100ng/mL of lipopolysaccharide (LPS) for six hours with 40 µM TJ-M2010-5 or vehicle one hour pretreatment, cells in individual wells were harvested for protein extraction.|
|Incubation time||6 hours|
|Animal models||Female BalB/c mice (6–8 weeks old)|
|Formulation||vehicle (ddH2 O)|
|Solubility (25°C)||DMSO 90 mg/mL|
|Storage||4°C, protect from light, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
 Zeyang Li, et al. Front Pharmacol. TJ-M2010-5, a novel CNS drug candidate, attenuates acute cerebral ischemia-reperfusion injury through the MyD88/NF-κB and ERK pathway
 Huifang Yang, et al. J Cardiovasc Transl Res. TJ-M2010-5 Attenuates Severe Myocardial Ischemia/Reperfusion Injury in Heart Transplantation by Inhibiting MyD88 Homodimerization In Vivo
 Yalong Xie, et al. Chem Biol Interact. TJ-M2010-5, A self-developed MyD88 inhibitor, attenuates liver fibrosis by inhibiting the NF-κB pathway
 Wei Zhou, et al. Int Immunopharmacol. Hypothermic oxygenated perfusion combined with TJ-M2010-5 alleviates hepatic ischemia-reperfusion injury in donation after circulatory death
 Yan Miao, et al. Am J Transl Res. Inhibition of MyD88 by a novel inhibitor reverses two-thirds of the infarct area in myocardial ischemia and reperfusion injury
 Zhimiao Zou, et al. Int Immunopharmacol. TJ-M2010-5, a novel MyD88 inhibitor, corrects R848-induced lupus-like immune disorders of B cells in vitro
 Lin Xie, et al. J Natl Cancer Inst. Targeting of MyD88 Homodimerization by Novel Synthetic Inhibitor TJ-M2010-5 in Preventing Colitis-Associated Colorectal Cancer
|Related Immunology/Inflammation Products|
Fucoxanthin is a carotenoid that occurs naturally in certain algae with anti-obesity, anti-oxidant, anti-diabetic, anticancer and anti-inflammatory activities.
MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
Loxoprofen Sodium is a nonsteroidal anti-inflammatory drug (NSAID) in the propionic acid derivatives group
PMX-53 is a potent CD88 (C5aR) antagonist that inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation.
Perflubron (1-Bromoperfluorooctane, Perfluorooctyl bromide, Oxygent, PFOB) exhibits anti-inflammatory activity thus decreases cytokine production in human alveolar macrophages. Perflubron also attenuates oxidative damage to both biological and nonbiological systems which is independent of its anti-inflammatory properties.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.