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Submit ReviewCRID3 sodium salt is a potent NLRP3 inflammasome inhibitor; closes the active conformation of NLRP3 to the inactive state. Directly interacts with the Walker B motif within the NLRP3 NACHT domain. Inhibits IL-1β, IL-18 and IL-1α production (IC50 values are 7.2, 10.3 and 12-18 nM, respectively). Selective for NLRP3 over NLRC4 inflammasome and Toll-like receptor signaling. Reduces severity of experimental autoimmune encephalomyelitis, skin inflammation and airway inflammation in mice. Also glutathione S-transferase omega 1 inhibitor. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
分子量 | 426.46 |
公式 | C20H23N2NaO5S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 256373-96-3 |
PubChem ID | 91826093 |
InChI Key | LFQQNXFKPNZRFT-UHFFFAOYSA-M |
Smiles | O=C(N(S(C4=CC(C(C)(O)C)=CO4)(=O)=O)[Na])NC1=C3C(CCC3)=CC2=C1CCC2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 42.65 | 100 | |
DMSO | 42.65 | 100 |
以下数据基于产品分子量 426.46。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.34 mL | 11.72 mL | 23.45 mL |
5 mM | 0.47 mL | 2.34 mL | 4.69 mL |
10 mM | 0.23 mL | 1.17 mL | 2.34 mL |
50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
参考文献是支持产品生物活性的出版物。
Laliberte et al (2003) Glutathione S-transferase omega 1-1 is a target of cytokine release inhibitory drugs and may be responsible for their effect on interleukin-1β posttranslational processing. J.Biol.Chem. 278 16567 PMID: 12624100
Coll et al (2015) A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat.Med. 21 248 PMID: 25686105
Gordon et al (2018) Inflammasome inhibition prevents a-synuclein pathology and dopaminergic neurodegeneration in mice. Sci.Transl.Med. 10 eaah4066 PMID: 30381407
Tapia-Abellán et al (2019) MCC950 closes the active conformation of NLRP3 to an inactive state. Nat.Chem.Biol. 15 560 PMID: 31086329
Coll et al (2019) MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition. Nat.Chem.Biol. 15 556 PMID: 31086327
If you know of a relevant reference for CRID3 sodium salt, please let us know.
关键词: CRID3 sodium salt, CRID3 sodium salt supplier, CP456773, cytokine, release, inhibitory, drug, CRID3, Glutathione, S-transferase, omega, 1, GSTO1, inhibitors, inhibits, MCC950, nod-like, receptors, NLRP3, inflammasome, CP-456773, MCC, 950, Other, Transferases, Cytokines, Inflammasomes, 5479, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CRID3 sodium salt 的部分引用包括:
David A et al (2022) Interleukin 38 alleviates aortic valve calcification by inhibition of NLRP3. Proc Natl Acad Sci U S A 119 e2202577119 PMID: 36037361
Flóra et al (2022) Maternal P2X7 receptor inhibition prevents autism-like phenotype in male mouse offspring through the NLRP3-IL-1β pathway. Brain Behav Immun 101 318-332 PMID: 35065198
Goddard et al (2019) Enteropathogenic Escherichia coli Stimulates Effector-Driven Rapid Caspase-4 Activation in Human Macrophages. Cell Rep 27 1008 PMID: 31018119
Oliver T et al (2020) CARD8 inflammasome activation triggers pyroptosis in human T cells. EMBO J 39 e105071 PMID: 32840892
Minqi et al (2020) Eldecalcitol Inhibits LPS-Induced NLRP3 Inflammasome-Dependent Pyroptosis in Human Gingival Fibroblasts by Activating the Nrf2/HO-1 Signaling Pathway. Drug Des Devel Ther 14 4901-4913 PMID: 33223823
Nagesh et al (2020) Inhibition of Amyloid-Beta Production, Associated Neuroinflammation, and Histone Deacetylase 2-Mediated Epigenetic Modifications Prevent Neuropathology in Alzheimer's Disease in vitro Model. Front Aging Neurosci 11 342 PMID: 32009938
Nitya et al (2020) Genetic and pharmacological inhibition of inflammasomes reduces the survival of Mycobacterium tuberculosis strains in macrophages. Sci Rep 10 3709 PMID: 32111888
Chauhan et al (2018) BAX/BAK-Induced Apoptosis Results in Caspase-8-Dependent IL-1β Maturation in Macrophages. Cell Rep 25 2354 PMID: 30485805
Eduardo et al (2021) An in vitro study of ApxI from Actinobacillus pleuropneumoniae serotype 10 and induction of NLRP3 inflammasome-dependent cell death. Vet Rec Open 8 e20 PMID: 34631111
Catherine B et al (2021) Inhibition of the NLRP3 inflammasome by HSP90 inhibitors. Immunology 162 84-91 PMID: 32954500
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.