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NLRP3 Inflammasome Inhibitor I

SKU: orb1225986

Description

It is a NLRP3 Inflammasome Inhibitor I.

Research Area

Immunology & Inflammation; Pharmacology & Drug Discovery; Cell Biology

Images & Validation

Key Properties

CAS Number16673-34-0
MW368.83
Purity>98% (HPLC)
FormulaC16H17ClN2O4S
SMILESO=C(NCCC1=CC=C(S(=O)(N)=O)C=C1)C2=CC(Cl)=CC=C2OC
TargetNOD
SolubilitySoluble in DMSO

Bioactivity

In Vivo
NLRP3-IN-2 is well tolerated with no effects on the glucose levels In vivo. NLRP3-IN-2 (100 mg/kg) treatment in a model of AMI due to ischemia+reperfusion significantly inhibits the activity of inflammasome (caspase-1) in the heart by 90% (P<0.01) and reduced infarct size, measured at pathology (by >40%, P<0.01) and with troponin I levels (by >70%, P<0.01). Animal model: Experimental acute myocardial infarction (AMI) model in mice. Dosage: 100 mg/kg. Administration: Intraperitoneal administration 30 minutes prior to surgery, then every 6 hours for 3 additional doses. Result: Led to a significant >90% reduction in caspase-1 activity (reflective of the formation of an active inflammasome) in the heart tissue measured 24 hours after ischemia. Led to a significant reduction in the infarct size measured with TTC (>40% reduction) or troponin I levels (>70% reduction) when compared with vehicle alone.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Glibenclamide impurity A | Glibenclamide A | Glyburide Related Compound A | NLRP3 Inflammasome Inhibitor I

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Protocol Information

NLRP3 Inflammasome Inhibitor I (orb1225986)

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% DMSO +
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% Tween 80 +
%

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500 mg
50 mg
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200 mg
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