Oclacitinib 1208319-26-9 High purity oclactinib
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) [1]
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) [1].
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 [2].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 [3].
Identification | ||||
Name | Oclacitinib | |||
Synonyms | JAKi; PF 03394197; trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanemethanesulfonamide | |||
Molecular Structure | ||||
Molecular Formula | C15H23N5O2S | |||
Molecular Weight | 337.44 | |||
CAS Registry Number | 1208319-26-9 | |||
Properties | ||||
Solubility | Sparingly Soluble (0.034 g/L) (25 ºC), Calc.* | |||
Density | 1.316±0.06 g/cm3 (20 ºC 760 Torr), Calc.* | |||
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