Stereochemistry | ACHIRAL |
Molecular Formula | C15H23N5O2S |
Molecular Weight | 337.44 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CNS(=O)(=O)C[C@H]1CC[C@@H](CC1)N(C)C2=C3C=CNC3=NC=N2
InChI
InChIKey=HJWLJNBZVZDLAQ-HAQNSBGRSA-N
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-
Molecular Formula | C15H23N5O2S |
Molecular Weight | 337.44 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Oclacitinib (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 as oclacitinib maleate is approved for control of pruritus associated with allergic dermatitis and control of atopic
dermatitis in dogs at least 12 months of age.
CNS Activity
Originator
Approval Year
PubMed
Patents
Sample Use Guides
Dogs: Oclacitinib, administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis.
Route of Administration:
Oral