product name Oclacitinib
Description: Oclacitinib (also known as PF-03394197) is a novel inhibitor of JAK family members with IC50 ranging from 10 to 99 nM and JAK1-dependent cytokines with IC50 ranging from 36 to 249 nM, which did not inhibit a panel of 38 non-JAK kinases. Oclacitinib is most potent at inhibiting JAK1. Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus.
References: Vet Dermatol. 2013 Oct;24(5):479-e114; J Vet Pharmacol Ther. 2014 Aug; 37(4): 317–324.
453.51
Formula
C15H23N5O2S.C4H4O4
CAS No.
1640292-55-2
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 90 mg/mL (198.5 mM)
Water: 18 mg/mL (39.7 mM)
Ethanol: 90 mg/mL (198.5 mM)
Solubility (In vivo)
Synonyms
PF-03394197
other peoduct :
| In Vitro |
In vitro activity: PF-03394197 inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. PF-03394197 is most potent at inhibiting JAK1. PF-03394197 also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 has minimal effects on cytokines which does not activate the JAK1 enzyme in cells. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | PF-03394197 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. PF-03394197 provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7. |
| Animal model | |
| Formulation & Dosage | |
| References | Vet Dermatol. 2013 Oct;24(5):479-e114; J Vet Pharmacol Ther. 2014 Aug; 37(4): 317–324. |
