MCC950 sodium (Synonyms: CRID3 sodium salt ) |
Catalog No.GC10634 |
MCC950 sodium (CP-456773 sodium ; sel de sodium CRID3) est un puissant inhibiteur sélectif de NLRP3 avec des IC50 de 7,5 et 8,1 nM dans les BMDM et HMDM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 256373-96-3
Sample solution is provided at 25 µL, 10mM.
MCC950 is a potent, selective, small molecule inhibitor of NLRP3. MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. MCC950 reduces Interleukin-1p (IL-1β) production in vivo and attenuates the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. Furthermore, MCC950 treatment rescues neonatal lethality in a mouse model of CAPS and is active in ex vivo samples from individuals with Muckle-Wells syndrome. MCC950 is thus a potential therapeutic for NLRP3-associated syndromes, including autoinflammatory and autoimmune diseases, and a tool for the further study of the NLRP3 inflammasome in human health and disease.[1]
The half-maximal inhibitory concentration (IC50) of MCC950 in BMDM was approximately 7.5 nM, while in HMDM it had a similar inhibitory capacity (IC50 = 8.1 nM). Cells were first primed with LPS then pre-treated with MCC950 and lastly stimulated with the NLRP3 stimulus ATP. Treating cells with nanomolar concentrations of MCC950 dose dependently inhibited the release of IL-1β in BMDM, HMDM and PBMC. [1]
Mice were pre-treated with MCC950 one hour before i.p. injection of LPS and were assessed two hours later. Pre-treatment with MCC950 reduced serum concentrations of IL-1β and IL-6 while it did not considerably decrease the amount of TNF-α, indicating that MCC950 is active in vivo.Besides, treatment of db/db mice with NLRP3 inflammasome inhibitor MCC950 ameliorated anxiety- and depression-like behaviors as well as cognitive dysfunction, and reversed increased NLRP3, ASC, and IL-1βexpression levels and caspase-1 activity in hippocampus. Moreover, MCC950 treatment significantly improved insulin sensitivity in db/db mice.[1,2]
References:
[1]. Coll, Rebecca C et al. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature medicine vol. 21,3 (2015): 248-55.
[2]. Zhai, Yadong et al. Inhibiting the NLRP3 Inflammasome Activation with MCC950 Ameliorates Diabetic Encephalopathy in db/db Mice. Molecules (Basel, Switzerland) vol. 23,3 522. 27 Feb. 2018.
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