5.38120
NLRP3 Inhibitor, MCC950
동의어(들):
NLRP3 Inhibitor, MCC950, N-(1,2,3,5,6,7-Hexahydro- s-indacen-4-ylcarbamoyl)-4-(2-hydroxy-2-propanyl)-2-furansulfonamide, Sodium, MCC-950, MCC950, Cytokine Release Inhibitory Drug 3, CRID 3, CP-456,773
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제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C20H23N2O5S · Na
CAS 번호:
Molecular Weight:
426.46
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
assay
≥97% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
water: 1 mg/mL, DMSO: 50 mg/mL
storage temp.
−20°C
SMILES string
[Na+].[S](=O)(=O)(N=C(Nc2c3c(cc4c2CCC4)CCC3)[O-])c1[o]cc(c1)C(O)(C)C
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
InChI key
LFQQNXFKPNZRFT-UHFFFAOYSA-M
General description
MCC950 is an antagonist ofInterleukin-1 beta (IL-1β). It interacts with both the inactive as well as active forms of NOD-like receptor protein 3 (NLRP3) and targets the Walker B motif within the NLRP3 NACHT domain. A cell-permeable, bioavailable, non-toxic sulfonylurea-derived compound that selectively interacts with the NLRP3 inflammasome and prevents its activation in a reversible manner with no effect on NLRC4 and NLRP1. Dose-dependently reduces IL-1β production (IC50 = 7.5 & 8.1 nM in LPS & ATP-treated BMDMs & HMDMs, respectively) with minimal effect on IL-1α & TNF-α. Specifically, it blocks NLRP3-dependent pyroptotic cell death by inhibiting caspase-1 &-11 activation, IL-1β processing, and ASC oligomerization. Does neither block K+ efflux, Ca2+ flux, or NLRP3-ASC interactions nor inhibits NLRC4, AIM2, TLR signaling, or NLRP3 priming. Effectively suppresses T cell responses and IL-1β& IL-6 secretion, reduces the severity of EAE, and rescues neonatal lethality in a mouse model of CAPS (10 mg/kg, i.p., q.d., & 20 mg/kg, i.p., every other day, respectively). Displays an attractive PK profile with desirable microsomal stability and minimal liability towards CYP450 isozymes (<15% inhibition at 10 µM) & hERG (IC50 >30 µM). It has demonstrated effectiveness against metabolic diseases, autoimmune diseases, cardiovascular diseases, and other conditions.
Application
MCC950 has been used in:
- hemolysis-affected mice to study the involvement of the NLRP3 inflammasome in kidney function injury.
- MCC950-mediated inflammasome inhibition assays.
- testing synergistic effect of pharmacologic inhibition of NLRP3 inflammasome in combination with immune checkpoint inhibitors (ICI) immunotherapy in tumor-bearing animals.
- studying the role of NLRP3 inflammasome in the development of endothelial dysfunction in early sepsis in mice.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
NLRP3
NLRP3
Reversible: yes
Packaging
Packaged under inert gas
Physical form
Supplied as a sodium salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Pleasenote that the molecular weight for this compound is batch-specific due tovariable water content. Please refer to the vial label or the certificate ofanalysis for the batch-specific molecular weight. The molecular weight providedrepresents the baseline molecular weight without water.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.