Product Description
- Potent, selective and orally available NLRP3 inflammasome inhibitor.
- Blocks the release of IL-1beta 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-1beta 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.
Recommended Use
Stable for at least 2 years after receipt when stored at -20°C.
References
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)
Purity : ≥97% (HPLC)
Product Type : Biochemicals
Host : Synthetic.
Solubility : Soluble in water, DMSO, dimethyl formamide or ethanol.
Storage & Handling : - 20°C