CY-09 is a selective and direct NLRP3 inhibitor to treat inflammatory disorders. CY-09 specifically blocks NLRP3 inflammasome activation in macrophages. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation. Importantly, treatment with CY-09 shows remarkable therapeutic effects on mouse models of cryopyrin-associated autoinflammatory syndrome (CAPS) and type 2 diabetes. Furthermore, CY-09 is active ex vivo for monocytes from healthy individuals or synovial fluid 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: ≥ 60 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.
GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor.
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.
|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.
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