Name | PF-03394197 Oclacitinib maleate |
Synonyms | PF-03394197 Oclacitinib Oclacitinib maleate PF-03394197 maleate VQIGDTLRBSNOBV-DYXOGNCHSA-N |
CAS | 1640292-55-2 |
Molecular Formula | C19H27N5O6S |
Molar Mass | 453.51258 |
Storage Condition | -20℃ |
In vitro study | PF-03394197 inhibits JAK family members with an IC50 of 10-99 nM and has little inhibitory effect on other non-JAK kinases. PF-03394197 is a very potent inhibitor of JAK1 and also inhibits the function of JAK1-dependent cytokines in several anti-allergic, inflammatory and pruritic responses. It has little effect on cytokines that are not involved in activating JAK1. |
In vivo study | Treatment by oral route at a PF-03394197 of 0.4-0.6 mg/kg twice a day is safe and effective for the treatment of pruritus due to allergic dermatitis. During the treatment period, the application of PF-03394197 alleviated itching within 24 hours, and in the experiment, more than 70% of the experimental animals (dogs) reduced the itching response by more than 50% on Day 7. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.205 ml | 11.025 ml | 22.05 ml |
5 mM | 0.441 ml | 2.205 ml | 4.41 ml |
10 mM | 0.221 ml | 1.103 ml | 2.205 ml |
5 mM | 0.044 ml | 0.221 ml | 0.441 ml |