Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF-α-induced necroptosis with EC50 of 490 nM. Necrostatin-1 is also an IDO inhibitor. Necrostatin-1 (Nec-1) efficiently inhibits the TNFα-induced necrotic death of L929 cells, which does not require exogenous caspase inhibitors. Necrostatin-1 (Nec-1) prevents radiocontrast media (RCM)-induced dilation of peritubular capillaries, suggesting a novel role unrelated to cell death for the RIP1 kinase domain in the regulation of microvascular hemodynamics and pathophysiology of contrast-induced AKI (CIAKI).
Anat Rec (Hoboken). 2020 Jan 21.
Cell Rep. 2020 May 19;31(7):107667.
hGBP1 Coordinates Chlamydia Restriction and Inflammasome Activation through Sequential GTP Hydrolysis
Necrostatin-1 purchased from AbMole
|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 39 mg/mL|
|Related RIPK Products|
|Necrostatin 2 racemate
Necrostatin-2 racemate (also known as 7-Cl-O-Nec-1 and Nec-1s) is a potent and specific receptor-interacting protein kinase 1 (RIPK1) inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
GSK547 is a potent and highly selective receptor-interacting serine/threonine protein kinase 1 (RIPK1) inhibitor.
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.
GSK2982772 is a potent and selective RIP1 (Receptor Interacting Protein 1) kinase inhibitor, with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively.
|GSK2983559 free acid
GSK2983559 free acid is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor.
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