Description:
Oclacitinib, also known as PF03394197, is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. Oclacitinib inhibited JAK family members by 50% at concentrations (IC50 's) ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nm). Oclacitinib was most potent at inhibiting JAK1 (IC50 = 10 nm). Oclacitinib also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50 's ranging from 36 to 249 nm. Oclacitinib had minimal effects on cytokines that did not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50 's > 1000 nm). These results demonstrate that oclacitinib is a targeted therapy that selectively inhibits JAK1-dependent cytokines involved in allergy, inflammation, and pruritus and suggests these are the mechanisms by which oclacitinib effectively controls clinical signs associated with allergic skin disease in dogs.
- Molecular Weight:337.44
- Melting Point:226-228°C
- Purity:98%
Molecular Formula:
C15H23N5O2S
Canonical SMILES:
CNS(=O)(=O)CC1CCC(CC1)N(C)C2=NC=NC3=C2C=CN3
InChI:
InChI=1S/C15H23N5O2S/c1-16-23(21,22)9-11-3-5-12(6-4-11)20(2)15-13-7-8-17-14(13)18-10-19-15/h7-8,10-12,16H,3-6,9H2,1-2H3,(H,17,18,19)/t11-,12-
InChIKey:
HJWLJNBZVZDLAQ-HAQNSBGRNA-N
Solubility:
Soluble in DMSO (Slightly), Methanol (Slightly, Sonicated)
Appearance:
Off-white to Pale Beige Solid
Storage: Store at 2-8°C under inert atmosphere
Synonyms:
Cyclohexanemethanesulfonamide, N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, trans-; trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexanemethanesulfonamide; JAKi; PF 03394197 Más detalles se encuentran
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