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iJak-381

Chemical Structure : iJak-381

CAS No.: 1831144-46-7

iJak-381 (iJak381)

Catalog No.: PC-35830Not For Human Use, Lab Use Only.

iJak-381 (iJak381) is a potent, selective inhalable and lung-restricted inhibitor of JAK1 with IC50 of 8.52 nM, displays 6.3/704/28 fold selectivity over JAK2/JAK3/TYK2.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

iJak-381 (iJak381) is a potent, selective inhalable and lung-restricted inhibitor of JAK1 with IC50 of 8.52 nM, displays 6.3/704/28 fold selectivity over JAK2/JAK3/TYK2.
iJak-381 suppresses STAT 6 activation by IL-1, suppresses ovalbumin-induced lung inflammation in both murine and guinea pig asthma models and improved allergen-induced airway hyperresponsiveness in mice.
In a model driven by human allergens, iJak-381 had a more potent suppressive effect on neutrophil-driven inflammation compared to systemic corticosteroid administration, reduces lung pathology without affecting systemic Jak1 activity in rodents.

Physicochemical Properties

M.Wt 612.039
Formula C28H28ClF2N9O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-(5-chloro-2-(difluoromethoxy)phenyl)-1-(2-(4-((2-cyanoethyl)(methyl)amino)piperidin-1-yl)-2-oxoethyl)-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

References

1. Dengler HS, et al. Sci Transl Med. 2018 Nov 21;10(468). pii: eaao2151. doi: 10.1126/scitranslmed.aao2151.

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