CAS NO: | 256373-96-3 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
200mg | 电议 |
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 |
Canonical SMILES | O=S([N-]C(NC1=C2CCCC2=CC3=C1CCC3)=O)(C4=CC(C(O)(C)C)=CO4)=O.[Na+] |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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.
Cell experiment:[1] | |
Cell lines | Bone marrow derived macrophages (BMDMs), human monocyte–derived macrophages (HMDMs), and human peripheral blood mononuclear cells (PBMCs) |
Reaction Conditions | 0.001 ~ 10 μM MCC950 sodium for 30 min incubation |
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] | |
Animal models | C57BL/6 mice |
Dosage form | 10 and 50 mg/kg Injected intraperitoneally (i.p.) |
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. |
Note | The technical data provided above is for reference only. |
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. |