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Oclacitinib Oclacitinib, also known as 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 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). These results demonstrate that oclacitinib is a targeted therapy that selectively inhibits JAK1-dependent cytokines involved in allergy, inflammation, and pruritus and suggests these are the mechanisms by which oclacitinib effectively controls clinical signs associated with allergic skin disease in dogs. Group: Pharmaceutical. Alternative Names: Cyclohexanemethanesulfonamide, N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, trans-; trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexanemethanesulfonamide; JAKi; PF 03394197. CAS No. 1208319-26-9. Pack Sizes: 50 mg. Product ID: B0084-462291. Molecular formula: C15H23N5O2S. Mole weight: 337.44. Custom synthesis BOC Sciences
London
Oclacitinib maleate Oclacitinib maleate was the first selective Janus kinase (JAK) inhibitor to be developed for dogs. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM). Group: Pharmaceutical. Alternative Names: Cyclohexanemethanesulfonamide, N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, trans-, (2Z)-2-butenedioate (1:x); Apoquel; Oclacitinib maleate (1:x); PF 03394197-11; trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexanemethanesulfonamide maleate (1:x); N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide maleate. CAS No. 1208319-27-0. Pack Sizes: 10 g. Product ID: B1370-007675. Molecular formula: C15H23N5O2S.xC4H4O4. Mole weight: 337.44 (free base). Custom synthesis is available. Send your inquiries for more information. BOC Sciences
London
Oclacitinib monomaleate Oclacitinib, also called as PF-03394197, is a novel inhibitor of JAK family members (IC50 = 10 - 99 nM) and JAK1-dependent cytokines involved in allergy, inflammation, and pruritus (IC50 = 36 - 249 nM), without affecting a panel of 38 non-JAK kinases. It could reduce pruritus and associated inflammatory skin lesions in dogs with AD. Group: Pharmaceutical. Alternative Names: Cyclohexanemethanesulfonamide, N-methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-, trans-, (2Z)-2-butenedioate (1:1); trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclohexanemethanesulfonamide maleate (1:1); N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide monomaleate. CAS No. 1640292-55-2. Pack Sizes: 50 mg. Product ID: B2693-008142. Molecular formula: C15H23N5O2S.C4H4O4. Mole weight: 453.51. Custom synthesis is available. Send your inquiries for more information. BOC Sciences
London

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