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MedKoo Cat#: 522637 | Name: CP-456773 sodium
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

CP-456773, also known as MCC950 and CRID3, is a potent and selective cytokine release inhibitor and NLRP3 inflammasome inhibitor for the treatment of inflammatory diseases. CP-456773 inhibits interleukin 1β (IL-1β) secretion and caspase 1 processing. MCC950 blocked canonical and noncanonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibited activation of NLRP3 but not the AIM2, NLRC4 or NLRP1 inflammasomes. MCC950 reduced interleukin-1β (IL-1β) production in vivo and attenuated the severity of experimental autoimmune encephalomyelitis (EAE), a disease model of multiple sclerosis. MCC950 is a potential therapeutic for NLRP3-associated syndromes, including autoinflammatory and autoimmune diseases, and a tool for further study of the NLRP3 inflammasome in human health and disease.

Chemical Structure

CP-456773 sodium
CP-456773 sodium
CAS#256373-96-3 (sodium)

Theoretical Analysis

MedKoo Cat#: 522637

Name: CP-456773 sodium

CAS#: 256373-96-3 (sodium)

Chemical Formula: C20H23N2NaO5S

Exact Mass: 0.0000

Molecular Weight: 426.46

Elemental Analysis: C, 56.33; H, 5.44; N, 6.57; Na, 5.39; O, 18.76; S, 7.52

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 150.00 Ready to ship
50mg USD 250.00 Ready to ship
100mg USD 450.00 Ready to ship
200mg USD 750.00 Ready to ship
500mg USD 1,650.00 Ready to ship
1g USD 2,950.00 Ready to ship
2g USD 5,250.00 2 Weeks
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Related CAS #
256373-96-3 (sodium) 210826-40-7 (free acid)
Synonym
MCC950; MCC 950; MCC-950; CP-456773; CP456773; CP 456773; CRID-3; CRID3; CRID 3; CP-456773 sodium salt; Cytokine release inhibitory drug 3
IUPAC/Chemical Name
sodium ((1,2,3,5,6,7-hexahydro-s-indacen-4-yl)carbamoyl)((4-(2-hydroxypropan-2-yl)furan-2-yl)sulfonyl)amide
InChi Key
LFQQNXFKPNZRFT-UHFFFAOYSA-M
InChi Code
InChI=1S/C20H24N2O5S.Na/c1-20(2,24)14-10-17(27-11-14)28(25,26)22-19(23)21-18-15-7-3-5-12(15)9-13-6-4-8-16(13)18;/h9-11,24H,3-8H2,1-2H3,(H2,21,22,23);/q;+1/p-1
SMILES Code
O=S(C1=CC(C(C)(O)C)=CO1)([N-]C(NC2=C3CCCC3=CC4=C2CCC4)=O)=O.[Na+]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
MCC950 ameliorates sewing machine oil-induced acute exogenous lipoid pneumonia in rats through inhibition of the NF-[Formula: see text]B/NLRP3 inflammasome pathway. MCC950 improves lipopolysaccharide‑induced systemic inflammation in mice by relieving pyroptosis in blood neutrophils. MCC950 Regulates Stem Cells Destiny Through Modulating SIRT3-NLRP3 Inflammasome Dynamics During Oxygen Glucose Deprivation
Biological target:
MCC950 sodium (CP-456773 sodium; CRID3 sodium salt) is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in mouse bone marrow derived macrophages and human monocyte derived macrophages, respectively.
In vitro activity:
MCC950 blocks canonical and non-canonical NLRP3 activation at nanomolar concentrations. MCC950 specifically inhibits NLRP3 but not AIM2, NLRC4 or NLRP1 activation. The effect of MCC950 on NLRP3 inflammasome activation is tested in mouse bone marrow derived macrophages (BMDM) and human monocyte derived macrophages (HMDM). The IC50 of MCC950 in BMDM is approximately 7.5 nM, while in HMDM it has a similar inhibitory capacity (IC50=8.1 nM). MCC950 also dose dependently inhibit IL-1β but not TNF-α secretion. MCC950 specifically blocks caspase-11-directed NLRP3 activation and IL-1β secretion upon stimulation of the non-canonical pathway. NLRC4-stimulated IL-1β and TNF-α secretion (as activated by Salmonella typhimurium) are not inhibited by MCC950 even at a concentration of 10 µM. MCC950 does not inhibit caspase-1 activation or IL-1β processing in response to S. typhimurium. The expression of pro-caspase-1 and pro-IL-1β in cell lysates is not substantially affected by MCC950 treatment. Reference: Nat Med. 2015 Mar;21(3):248-55. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4392179/
In vivo activity:
Treatment with MCC950 (10 mg/kg) was efficacious in ameliorating anxiety-like behaviors in L/D box, depression-like behaviors in TST and FST, cognitive disorders in MWM test, as well as decreasing hippocampal NLRP3, ASC, and IL-1β expression levels and caspase-1 activity in db/db mice. Additionally, the plasma IL-1β level was significantly reduced after 12 weeks treatment of MCC950. Interestingly, MCC950 treatment failed to inhibit the increase of TNF-α level in plasma and hippocampus of db/db mice. The effect of MCC950 treatment on decreasing IL-1β level in db/db mice was stronger than that of TNF-α, demonstrating that the inhibition of IL-1β secretion was specific. MCC950 treatment could improve insulin sensitivity in db/db mice, which might result from inhibiting NLRP3 inflammasome activation. Reference: Molecules. 2018 Feb 27;23(3):522. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017493/
Solvent mg/mL mM
Solubility
Soluble in DMSO 50.0 117.24
Water 30.0 70.35
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 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.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Gritsenko A, Yu S, Martin-Sanchez F, Diaz-Del-Olmo I, Nichols EM, Davis DM, Brough D, Lopez-Castejon G. Priming Is Dispensable for NLRP3 Inflammasome Activation in Human Monocytes In Vitro. Front Immunol. 2020 Sep 30;11:565924. doi: 10.3389/fimmu.2020.565924. PMID: 33101286; PMCID: PMC7555430. 2. Zhang Y, Lv X, Hu Z, Ye X, Zheng X, Ding Y, Xie P, Liu Q. Protection of Mcc950 against high-glucose-induced human retinal endothelial cell dysfunction. Cell Death Dis. 2017 Jul 20;8(7):e2941. doi: 10.1038/cddis.2017.308. PMID: 28726778; PMCID: PMC5550855. 3. Coll RC, Robertson AA, Chae JJ, Higgins SC, Muñoz-Planillo R, Inserra MC, Vetter I, Dungan LS, Monks BG, Stutz A, Croker DE, Butler MS, Haneklaus M, Sutton CE, Núñez G, Latz E, Kastner DL, Mills KH, Masters SL, Schroder K, Cooper MA, O'Neill LA. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015 Mar;21(3):248-55. doi: 10.1038/nm.3806. Epub 2015 Feb 16. PMID: 25686105; PMCID: PMC4392179. 4. Zhai Y, Meng X, Ye T, Xie W, Sun G, Sun X. Inhibiting the NLRP3 Inflammasome Activation with MCC950 Ameliorates Diabetic Encephalopathy in db/db Mice. Molecules. 2018 Feb 27;23(3):522. doi: 10.3390/molecules23030522. PMID: 29495433; PMCID: PMC6017493.
In vitro protocol:
1. Gritsenko A, Yu S, Martin-Sanchez F, Diaz-Del-Olmo I, Nichols EM, Davis DM, Brough D, Lopez-Castejon G. Priming Is Dispensable for NLRP3 Inflammasome Activation in Human Monocytes In Vitro. Front Immunol. 2020 Sep 30;11:565924. doi: 10.3389/fimmu.2020.565924. PMID: 33101286; PMCID: PMC7555430. 2. Zhang Y, Lv X, Hu Z, Ye X, Zheng X, Ding Y, Xie P, Liu Q. Protection of Mcc950 against high-glucose-induced human retinal endothelial cell dysfunction. Cell Death Dis. 2017 Jul 20;8(7):e2941. doi: 10.1038/cddis.2017.308. PMID: 28726778; PMCID: PMC5550855.
In vivo protocol:
1. Coll RC, Robertson AA, Chae JJ, Higgins SC, Muñoz-Planillo R, Inserra MC, Vetter I, Dungan LS, Monks BG, Stutz A, Croker DE, Butler MS, Haneklaus M, Sutton CE, Núñez G, Latz E, Kastner DL, Mills KH, Masters SL, Schroder K, Cooper MA, O'Neill LA. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nat Med. 2015 Mar;21(3):248-55. doi: 10.1038/nm.3806. Epub 2015 Feb 16. PMID: 25686105; PMCID: PMC4392179. 2. Zhai Y, Meng X, Ye T, Xie W, Sun G, Sun X. Inhibiting the NLRP3 Inflammasome Activation with MCC950 Ameliorates Diabetic Encephalopathy in db/db Mice. Molecules. 2018 Feb 27;23(3):522. doi: 10.3390/molecules23030522. PMID: 29495433; PMCID: PMC6017493.
1. Lipopolysaccharide (LPS) stimulation of Pancreatic Ductal Adenocarcinoma (PDAC) and macrophages activates the NLRP3 inflammasome that influences the levels of pro-inflammatory cytokines in a co-culture model. Sivam HGP, Chin BY, Gan SY, Ng JH, Gwenhure A, Chan EWL. Cancer Biol Ther. 2023 Dec 31;24(1):2284857. doi: 10.1080/15384047.2023.2284857. Epub 2023 Nov 29. PMID: 38018872 2. Molecular mechanisms underlying NLRP3 inflammasome activation and IL-1β production in air pollution fine particulate matter (PM2.5)-primed macrophages. Caceres L, Abogunloko T, Malchow S, Ehret F, Merz J, Li X, Sol Mitre L, Magnani N, Tasat D, Mwinyella T, Spiga L, Suchanek D, Fischer L, Gorka O, Colin Gissler M, Hilgendorf I, Stachon P, Rog-Zielinska E, Groß O, Westermann D, Evelson P, Wolf D, Marchini T. Environ Pollut. 2023 Nov 22:122997. doi: 10.1016/j.envpol.2023.122997. Online ahead of print. PMID: 38000727 3. Selective inhibition of the NLRP3 inflammasome protects against acute ethanol-induced cardiotoxicity in an FBXL2-dependent manner. Yuan M, Ceylan AF, Gao R, Zhu H, Zhang Y, Ren J. Acta Biochim Biophys Sin (Shanghai). 2023 Nov 22. doi: 10.3724/abbs.2023256. Online ahead of print. PMID: 37994158 Free article. 4 Cite Share Caspase-1 Responsive Nanoreporter for In Vivo Monitoring of Inflammasome Immunotherapy. Nandi D, Forster Iii J, Ramesh A, Nguyen A, Bharadwaj H, Kulkarni A. ACS Appl Mater Interfaces. 2023 Nov 22. doi: 10.1021/acsami.3c15733. Online ahead of print. PMID: 37990965 5 Cite Share Lupeol alleviates autoimmune myocarditis by suppressing macrophage pyroptosis and polarization via PPARα/LACC1/NF-κB signaling pathway. Xiong Y, Zhang Z, Liu S, Shen L, Zheng L, Ding L, Liu L, Wu L, Li L, Hu Z, Zhang Z, Zhou L, Yao Y. Phytomedicine. 2023 Nov 8;123:155193. doi: 10.1016/j.phymed.2023.155193. Online ahead of print. PMID: 37976692 Free article. 6 Cite Share The role and mechanism of inflammatory response to growing rod implantation in early onset scoliosis. Zhang H, Han B, Li Z, Zhao Y, Du Y, Yang Y, Wang S, Zhang J. Front Cell Dev Biol. 2023 Oct 26;11:1282573. doi: 10.3389/fcell.2023.1282573. eCollection 2023. PMID: 37965575 Free PMC article. Review. 7 Cite Share Intraperitoneal Injection of MCC950 Inhibits the Progression of Myopia in Form-Deprivation Myopic Mice. Chen Z, Xiao K, Long Q. Int J Mol Sci. 2023 Oct 31;24(21):15839. doi: 10.3390/ijms242115839. PMID: 37958819 Free PMC article. Item in Clipboard 8 Cite Share Aggregated Hendra virus C-protein activates the NLRP3 inflammasome to induce inflammation. Barry K, Harpur C, Lam M, Tate MD, Mansell A. J Inflamm (Lond). 2023 Nov 10;20(1):38. doi: 10.1186/s12950-023-00365-8. PMID: 37950278 Free PMC article. 9 Cite Share FoxO1 knockdown inhibits RANKL-induced osteoclastogenesis by blocking NLRP3 inflammasome activation. Wang Z, Luo W, Zhang G, Li H, Zhou F, Wang D, Feng X, Xiong Y, Wu Y. Oral Dis. 2023 Nov 5. doi: 10.1111/odi.14800. Online ahead of print. PMID: 37927112 10 Cite Share MCC950 Ameliorates Acute Exogenous Lipoid Pneumonia Induced by Sewing Machine Oil in Rats via the NF-κB/NLRP3 Inflammasome Pathway. Ye WD, Wang HM, Xu ZJ, Liang DS, Huang AR, Xu ZW, Hu XG, Jin YM. In Vivo. 2023 Nov-Dec;37(6):2533-2542. doi: 10.21873/invivo.13361. PMID: 37905651 Free PMC article. Item in Clipboard 11 Cite Share Hydrogen sulfide ameliorates lipopolysaccharide-induced anxiety-like behavior by inhibiting checkpoint kinase 1 activation in the hippocampus of mice. Shentu Y, Chen M, Wang H, Du X, Zhang W, Xie G, Zhou S, Ding L, Zhu Y, Zhu M, Zhang N, Du C, Ma J, Chen R, Yang J, Fan X, Gong Y, Zhang H, Fan J. Exp Neurol. 2023 Oct 26;371:114586. doi: 10.1016/j.expneurol.2023.114586. Online ahead of print. PMID: 37898396 12 Cite Share Glycine-Alanine Dipeptide Repeat Protein from C9-ALS Interacts with Sulfide Quinone Oxidoreductase (SQOR) to Induce the Activity of the NLRP3 Inflammasome in HMC3 Microglia: Irisflorentin Reverses This Interaction. Fu RH, Chen HJ, Hong SY. Antioxidants (Basel). 2023 Oct 23;12(10):1896. doi: 10.3390/antiox12101896. PMID: 37891975 Free PMC article. 13 Cite Share High-dose remifentanil exacerbates myocardial ischemia-reperfusion injury through activation of calcium-sensing receptor-mediated pyroptosis. Zhu Y, Chi J, Cai S, Liu S, Yuan J, Xu H, Zhou H. Int J Med Sci. 2023 Sep 18;20(12):1570-1583. doi: 10.7150/ijms.83207. eCollection 2023. PMID: 37859698 Free PMC article. 14 Cite Share NLRP3-inflammasome inhibition by MCC950 attenuates cardiac and pulmonary artery remodelling in heart failure with preserved ejection fraction. Cheng X, Zhao H, Wen X, Li G, Guo S, Zhang D. Life Sci. 2023 Nov 15;333:122185. doi: 10.1016/j.lfs.2023.122185. Epub 2023 Oct 17. PMID: 37858713 Item in Clipboard 15 Cite Share Interrogating direct NLRP3 engagement and functional inflammasome inhibition using cellular assays. Teske KA, Corona C, Wilkinson J, Mamott D, Good DA, Zambrano D, Lazar DF, Cali JJ, Robers MB, O'Brien MA. Cell Chem Biol. 2023 Oct 12:S2451-9456(23)00335-5. doi: 10.1016/j.chembiol.2023.09.016. Online ahead of print. PMID: 37858335 Free article. 16 Cite Share CTRP3 inhibits myocardial fibrosis through the P2X7R-NLRP3 inflammasome pathway in SHR rats. Liu N, Gong Z, Li Y, Xu Y, Guo Y, Chen W, Sun X, Yin X, Liu W. J Hypertens. 2023 Oct 10. doi: 10.1097/HJH.0000000000003591. Online ahead of print. PMID: 37850974 17 Cite Share Selective Immunosuppression Targeting the NLRP3 Inflammasome Mitigates the Foreign Body Response to Implanted Biomaterials While Preserving Angiogenesis. Chan AHP, Moore MJ, Grant AJ, Lam YTM, Darnell MV, Michael PL, Wise SG, Tan RP. Adv Healthc Mater. 2023 Oct 17:e2301571. doi: 10.1002/adhm.202301571. Online ahead of print. PMID: 37846971 18 Cite Share Sorcin regulate pyroptosis by interacting with NLRP3 inflammasomes to facilitate the progression of hepatocellular carcinoma. Li Z, Yang Z, Zhu Y, Fu C, Li N, Peng F. Cell Death Dis. 2023 Oct 13;14(10):678. doi: 10.1038/s41419-023-06096-1. PMID: 37833249 Free PMC article. 19 Cite Share Neuritin has a neuroprotective role in the rat model of acute ischemia stroke by inhibiting neuronal apoptosis and NLRP3 inflammasome. Xu H, Dong J, Li Y, Zhang L, Yin J, Zhu C, Wang X, Ren K, Zhang H, Zhao D. J Stroke Cerebrovasc Dis. 2023 Dec;32(12):107391. doi: 10.1016/j.jstrokecerebrovasdis.2023.107391. Epub 2023 Oct 11. PMID: 37832268 20 Cite Share Staphylococcus aureus enhances osteoclast differentiation and bone resorption by stimulating the NLRP3 inflammasome pathway. Yao L, Huang C, Dai J. Mol Biol Rep. 2023 Nov;50(11):9395-9403. doi: 10.1007/s11033-023-08900-9. Epub 2023 Oct 11. PMID: 37817024