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MCC950 sodium salt (CP-456773)

Cat. No. M8083
MCC950 sodium salt (CP-456773) Structure
Synonym:

CP-456773 sodium; CRID3 sodium salt

Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 85  USD85 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

MCC950 (CP-456773) sodium salt is a potent, selective NLRP3 inhibitor with IC50s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively. MCC950 (CP-456773) sodium salt inhibits interleukin 1β (IL-1β) secretion and caspase 1 processing.

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.

Product Citations
Customer Product Validations & Biological Datas
Source Journal of Immunology Research (2018). Figure 6. MCC950 (Abmole Bioscience, USA)
Method i.p.
Cell Lines mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results More interestingly, we found that sevoflurane abolished the OVA-induced expression of NLRP3, which is similar to that observed in MCC950-treated allergic mice.
Source Journal of Immunology Research (2018). Figure 5. MCC950 (Abmole Bioscience, USA)
Method i.p.
Cell Lines mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results As expected, OVA challenge significantly increased the production of serum IgE compared with that of the control groups. Sevoflurane or MCC950 treatment significantly decreased OVA-induced IgE levels, although these levels remained higher than those in the control mice
Source Journal of Immunology Research (2018). Figure 4. MCC950 (Abmole Bioscience, USA)
Method i.p.
Cell Lines mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results Sevoflurane or MCC950 treatment resulted in a marked reduction in goblet cell hyperplasia (Figures 4(a)-4(f))
Source Journal of Immunology Research (2018). Figure 3. MCC950 (Abmole Bioscience, USA)
Method i.p.
Cell Lines mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results Treatment with sevoflurane or MCC950 produced a profound reduction in the total numbers and differential counts of inflammatory cells in BALF
Source Journal of Immunology Research (2018). Figure 2. MCC950 (Abmole Bioscience, USA)
Method i.p.
Cell Lines mice
Concentrations 10 mg/kg
Incubation Time 24 h
Results OVA challenge significantly increased the inflammatory cells concentrated near the airways (Figure 2(c)), while sevoflurane or MCC950 treatment resulted in a marked decrease in inflammatory cell infiltration (Figures 2(d)-2(f)).
Source Neural Plast (2018). Figure 3. MCC950
Method i.p
Cell Lines mice
Concentrations 50 mg/kg
Incubation Time 24 hr
Results When compared with the vehicle group, MCC950, the NLRP3 inhibitor significantly reduced the neurological deficit score 24 hr after cerebral ischemia reperfusion in diabetic mice
Chemical Information
Molecular Weight 426.46
Formula C20H23N2NaO5S
CAS Number 256373-96-3
Solubility (25°C) Water 30 mg/mL
DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yifan Wang, et al. Biomed Res Int. Overexpression of Limb Bud and Heart Alleviates Sepsis-Induced Acute Lung Injury via Inhibiting the NLRP3 Inflammasome

[2] Hui Yin, et al. Anat Rec (Hoboken). Resibufogenin suppresses growth and metastasis through inducing caspase-1-dependent pyroptosis via ROS-mediated NF-κB suppression in non-small cell lung cancer

[3] Qinyu Wang, et al. Br J Pharmacol. Naringenin attenuates non-alcoholic fatty liver disease by down-regulating the NLRP3/NF-κB pathway in mice

[4] Cong-Fa Huang, et al. J Exp Clin Cancer Res. NLRP3 inflammasome activation promotes inflammation-induced carcinogenesis in head and neck squamous cell carcinoma

[5] Dempsey C, et al. Brain Behav Immun. Inhibiting the NLRP3 inflammasome with MCC950 promotes non-phlogistic clearance of amyloid-β and cognitive function in APP/PS1 mice.

[6] Salla M, et al. ACS Med Chem Lett. dentification, Synthesis, and Biological Evaluation of the Major Human Metabolite of NLRP3 Inflammasome Inhibitor MCC950.

[7] Rebecca C Coll, et al. Nat Med. A small-molecule inhibitor of the NLRP3 inflammasome for the treatment of inflammatory diseases

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Keywords: MCC950 sodium salt (CP-456773), CP-456773 sodium; CRID3 sodium salt supplier, Pyroptosis, inhibitors, activators


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