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INF39

Cat. No. M9516
INF39 Structure
Synonym:

INF-39

Size Price Availability Quantity
5mg USD 165  USD165 In stock
10mg USD 255  USD255 In stock
25mg USD 565  USD565 In stock
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Quality Control & Documentation
Biological Activity

INF39 is a nontoxic, irreversible NLRP3 inhibitor able to decrease interleukin-1β release from macrophages. INF39 (INF39) significantly inhibits ATP- and nigericin-induced IL-1β release. INF39 potentially reacts with Cys-SH residues in the active site of cysteine protease caspase-1, but does not directly target caspase-1 activity. The inhibition of NLRP3 inflammasome complex with INF39 dose-dependently attenuates the decrease in colonic length (-19, -13 and -8% at 12.5, 25, 50 mg/kg, respectively). Rats treated with INF39 displays a significant reduction of macroscopic damage score (4.7 at 12.5 mg/kg, 3.1 at 25 mg/kg, and 2.8 at 50 mg/kg). Oral administration of INF39 reduces colonic myeloperoxidase, IL-1β, and TNF Levels in DNBS-treated rats.

<span style='color:#ff0000;'><strong>*The compound is unstable in solutions, freshly prepared is recommended</strong></span>


Chemical Information
Molecular Weight 224.68
Formula C12H13ClO2
CAS Number 866028-26-4
Solubility (25°C) DMSO
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] Cocco M, et al. J Med Chem. Development of an Acrylate Derivative Targeting the NLRP3 Inflammasome for the Treatment of Inflammatory Bowel Disease.

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  Catalog
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Keywords: INF39, INF-39 supplier, NLR, inhibitors, activators


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