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|
|Related NLR Products|
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.
Dapansutrile (OLT1177) is a first-in-class potent, selective and orally active inhibitor of NLRP3 inflammasome.
CY-09 is a selective and direct NLRP3 inhibitor.
|MCC950 sodium salt (CP-456773)
MCC950 (CP-456773) sodium salt was found to act as a cytokine release inhibitory drug and inhibitor of the NLRP3 inflammasome.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.