GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 blocks synergy between NOD2 and TLR2. GSK717 does not affect NOD1, TNFR1 and TLR2-mediated responses. GSK717 (5 μM) inhibits the release of IL-8, IL-6, TNFα and IL-1β in primary human monocytes stimulated with MDP. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells.
|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.
|Solubility||DMSO ≥ 100 mg/mL|
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Trimethylamine n-oxide is a microbiome dependent metabolite of dietary choline and other Trimethylamine nutrients. It belongs to the amine oxide class. Trimethylamine n-oxide induces inflammation by activating the ROS/NLRP3 inflammasome. Trimethylamine n-oxide also accelerates fibroblast differentiation and induces cardiac fibrosis by activating the TGF-β/smad2 signaling pathway.
JC124 IS A SPECIFIC INHIBITOR OF THE NLRP3 INFLAMMASOME. JC124 HAS ANTI-INFLAMMATORY AND NEUROPROTECTIVE EFFECTS.
Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species (ROS) and depress ER stress-mediated NOD activation.
INF39 is a nontoxic, irreversible NLRP3 inhibitor able to decrease interleukin-1β release from macrophages. *The compound is unstable in solutions, freshly prepared is recommended
Dapansutrile (OLT1177) is a first-in-class potent, selective and orally active inhibitor of NLRP3 inflammasome.
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