Cas No.: | 1640292-55-2 |
Chemical Name: | Oclacitinib maleate |
Synonyms: | Oclacitinib maleate;VQIGDTLRBSNOBV-DYXOGNCHSA-N;PF-03394197 maleate |
SMILES: | S(C([H])([H])C1([H])C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])N(C([H])([H])[H])C1C2C([H])=C([H])N([H])C=2N=C([H])N=1)(N([H])C([H])([H])[H])(=O)=O.O([H])C(/C(/[H])=C(/[H])\C(=O)O[H])=O |
Formula: | C19H27N5O6S |
M.Wt: | 453.512583017349 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Oclacitinib(PF03394197) is a potent and selective JAKs inhibitor with IC50 of 10-99 nM; not inhibit a panel of 38 non-JAK kinases (IC50 's > 1000 nM). IC50 value: 10 nM (JAK1) Target: JAKs in vitro: Oclacitinib 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) . in vivo: Dogs were randomized to receive either oclacitinib (0.4-0.6 mg/kg twice daily for 14 days and then once daily for up to 112 days) or an excipient-matched placebo .Dogs were randomized to either oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) was used by the owners to assess the severity of pruritus from day 0 to 7 and by veterinarians to assess the severity of dermatitis on days 0 and 7. Dogs could remain on the study for 28 days . For the detailed information of PF-03394197, the solubility of PF-03394197 in water, the solubility of PF-03394197 in DMSO, the solubility of PF-03394197 in PBS buffer, the animal experiment (test) of PF-03394197, the cell expriment (test) of PF-03394197, the in vivo, in vitro and clinical trial test of PF-03394197, the EC50, IC50,and Affinity of PF-03394197, Please contact DC Chemicals. |