MCC950 . sodium salt
50 CHF CHF 50.00
AG-CR1-3615-M0011 mgCHF 50.00
AG-CR1-3615-M0055 mgCHF 90.00
AG-CR1-3615-M01010 mgCHF 140.00
|Synonyms||MCC950; CP-456,773; CRID3; 1-(1,2,3,5,6,7-Hexahydro- s-indacen-4-yl)-3-[4-(1-hydroxy-1-methyl-ethyl)-furan-2-sulfonyl]urea|
|Purity Chemicals||≥97% (HPLC)|
|Solubility||Soluble in water (10mg/ml), DMSO (10mg/ml), dimethyl formamide or ethanol (1mg/ml).|
|Identity||Determined by 1H-NMR.|
|Shipping and Handling|
|Short Term Storage||+4°C|
|Long Term Storage||-20°C|
|Handling Advice||Keep cool and dry.|
|Use/Stability||Stable for at least 2 years after receipt when stored at -20°C.|
|Product Specification Sheet|
- Potent, selective and orally available NLRP3 inflammasome inhibitor.
- Blocks the release of IL-1β in macrophages primed with LPS and activated with ATP or nigericin, but it does not inhibit NLRP1, NLRC4, AIM2, TLR2 signaling or priming of NLRP3.
- Prevents oligomerization of ASC in cells stimulated with LPS and nigericin.
- Active in vivo, blocking the production of IL-1β and enhancing survival in mouse models of multiple sclerosis and cryopyrin-associated periodic syndrome (CAPS). Also active in ex vivo samples from individuals with Muckle-Wells syndrome.
- Potential therapeutic agent for NLRP3-associated syndromes, including autoinflammatory and autoimmune diseases.
- Glutathione s-transferase omega 1-1 is a target of cytokine release inhibitory drugs and may be responsible for their effect on interleukin-1beta posttranslational processing: R.E. Laliberte, et al.; J. Biol. Chem. 278, 16567 (2003)
- Novel synthesis of 1-(1,2,3,5,6,7-hexahydro-s-indacen-4-yl)-3-[4-(1-hydroxy-1-methylethyl)furan-2-sulfonyl]urea, an antiinflammatory agent: F.J. Urban, et al.; Synth. Commun. 33, 2029 (2003)
- The cytokine release inhibitory drug CRID3 targets ASC oligomerisation in the NLRP3 and AIM2 inflammasomes: R.C. Coll, et al.; PLoS One 6, e29539 (2011)
- A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases: R.C. Coll, et al.; Nat. Med. 21, 248 (2015)
- Taming the inflammasome: M. Levy, et al.; Nat. Med. 21, 213 (2015)
- The Nlrp3 inflammasome admits defeat: C.J. Gross & O. Gross; Trends Immunol. 36, 323 (2015)
- P2X7 receptor antagonism prevents IL-1β release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy: M.G. Khalafalla, et al.; J. Biol. Chem. 292, 16626 (2017)
- Inhibition of the NOD-like receptor protein 3 inflammasome Is protective in juvenile influenza A virus infection: B.M. Coates, et al.; Front. Immunol. 8, 782 (2017)
- MCC950, the selective NLRP3 inflammasome inhibitor protects mice against traumatic brain injury: S. Ismael, et al.; J. Neurotrauma 35,1294 (2017)
- Inhibitory Effect and Mechanism of Arctium lappa Extract on NLRP3 Inflammasome Activation: Y.K. Kim, et al.; Evid. Compl. Altern. Med. 6346734 (2018)
- MCC950, a specific small molecule inhibitor of NLRP3 inflammasome attenuates colonic inflammation in spontaneous colitis mice: A.P. Perera, et al.; Sci. Rep. 8, 8618 (2018)
- α1-antitrypsin mitigates NLRP3-inflammasome activation in amyloid β1–42-stimulated murine astrocytes: T. Ebrahimi, et al.; J. Neuroinfl. 15, 282 (2018)
- Pyrin dephosphorylation is sufficient to trigger inflammasome activation in familial Mediterranean fever patients: F. Magnotti, et al.; EMBO Mol. Med. 11, e10547 (2019)
- Toxoplasma gondii activates a Syk-CARD9-NF-κB signaling axis and gasdermin D-independent release of IL-1β during infection of primary human monocytes: W.J. Pandori, et al.; PLoS Pathog. 15, e1007923 (2019)