MCC950 sodium
MCC950 sodium salt is a potent, selective inhibitor of NOD-like receptor family protein 3 (NLRP3) with IC50 value of 7.5 nM in bone marrow derived macrophages (BMDMs) [1].
MCC950 effectively and selectively inhibits NLRP3 which is involved in various biological processes including autoinflammatory and autoimmune diseases. MCC950 is thus a potential therapeutic for NLRP3-associated syndromes, and a tool for the further study of the NLRP3 inflammasome in human health and disease [1].
In BMDM and human monocyte derived macrophage (HMDM) cells, MCC950 specifically inhibited canonical and noncanonical NLRP3 activation at IC50 of 7.5 nM and 8.1 nM, respectively, without affecting absent in melanoma 2 (AIM2), NOD-like receptor family CARD domain containing protein 4 (NLRC4) or NLRP1 inflammasomes [1].
In mice intraperitoneally injected with lipopolysaccharides (LPS), pre-treatment with MCC950 (50 mg/kg, i.p., 1 h before LPS injection) reduced serum concentrations of interleukin-1β (IL-1β) and IL-6 while it did not considerably decrease the amount of tumor necrosis factor-α (TNF-α). MCC950 attenuated the severity of experimental autoimmune encephalomyelitis [1].
Reference:
[1]. Coll R C, Robertson A A, Chae J J. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature Medicine, 2015, 21(3): 248-255.
- 1. Linkang Zhou, Xiaoxue Qiu, et al. "Hepatic danger signaling triggers TREM2+ macrophage induction and drives steatohepatitis via MS4A7-dependent inflammasome activation." Sci Transl Med. 2024 Mar 13;16(738):eadk1866. PMID: 38478630
- 2. Longfei Du, Xuyuan Fan, et al. "Quercetin Ameliorates Cognitive Impairment in Depression by Targeting HSP90 to Inhibit NLRP3 Inflammasome Activation." Mol Neurobiol. 2024 Feb 8. PMID: 38329680
- 3. Chaohong Li, Zhen Zhao, et al. "NLRP3-GSDMD-dependent IL-1β Secretion from Microglia Mediates Learning and Memory Impairment in a Chronic Intermittent Hypoxia-induced Mouse Model." Neuroscience. 2024 Feb 16:539:51-65. PMID: 38154620
- 4. Abbie Tomes, BSc (Hons), et al. "Activation of the inflammasome in bovine mammary macrophages by Streptococcus uberis." University of Nottingham, September 2023.
- 5. Yejing Zhu, Jinyu Chi, et al. "High-dose remifentanil exacerbates myocardial ischemia-reperfusion injury through activation of calcium-sensing receptor-mediated pyroptosis." Int J Med Sci. 2023 Sep 18;20(12):1570-1583. PMID: 37859698
- 6. Jiaxin He, Jialin Cui, et al. "Astragaloside IV Attenuates High-Glucose-Induced Impairment in Diabetic Nephropathy by Increasing Klotho Expression via the NF-κB/NLRP3 Axis." J Diabetes Res. 2023 May 22:2023:7423661. PMID: 37261217
| Storage | Store at -20°C |
| M.Wt | 426.46 |
| Cas No. | 256373-96-3 |
| Formula | C20H23N2NaO5S |
| Synonyms | CRID3 sodium salt |
| Solubility | ≥124 mg/mL in H2O; ≥21.45 mg/mL in DMSO; ≥43 mg/mL in EtOH |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | O=S([N-]C(NC1=C2CCCC2=CC3=C1CCC3)=O)(C4=CC(C(O)(C)C)=CO4)=O.[Na+] |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Bone marrow derived macrophages (BMDMs), human monocyte–derived macrophages (HMDMs), and human peripheral blood mononuclear cells (PBMCs) |
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Reaction Conditions |
0.001 ~ 10 μM MCC950 sodium for 30 min incubation |
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Applications |
Treating cells with nanomolar concentrations of MCC950 sodium dose-dependently inhibited the release of interleukin-1β (IL-1β) in BMDMs, HMDMs, and PBMCs. LPS-dependent tumor necrosis factor-α (TNF-α) secretion was not impaired by MCC950 sodium, which demonstrated that the inhibition effect of MCC950 sodium on IL-1β secretion was specific. |
| Animal experiment:[1] | |
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Animal models |
C57BL/6 mice |
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Dosage form |
10 and 50 mg/kg Injected intraperitoneally (i.p.) |
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Applications |
In mice intraperitoneally injected with lipopolysaccharides (LPS), pre-treatment with MCC950 sodium (50 mg/kg, i.p., 1 h before LPS injection) reduced serum concentrations of IL-1β and IL-6 while it did not considerably decrease the amount of TNF-α. Furthermore, MCC950 sodium (10 mg/kg, i.p.) attenuated the severity of experimental autoimmune encephalomyelitis, a disease model of multiple sclerosis. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Coll RC, Robertson AA, Chae JJ. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases. Nature Medicine, 2015, 21(3): 248-255. |
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Quality Control & MSDS
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Chemical structure
