- Oclacitinib
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- $0.00 / 1g
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2024-07-25
- CAS:1208319-26-9
- Min. Order: 1g
- Purity: 98%min
- Supply Ability: 10000g
- Oclacitinib
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- $50.00 / 1KG
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2023-12-23
- CAS:1208319-26-9
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: g-kg-tons, free sample is available
- Oclactinib
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- $100.00/ kg
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2023-06-16
- CAS:1208319-26-9
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 500t/month
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| | Oclacitinib Basic information |
| Product Name: | Oclacitinib | | Synonyms: | PF-03394197 (oclacitinib);Oclacitinib PF-03394197;JAKi;trans-N-Methyl-4-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-cyclohexanemethanesulfonamide;CyclohexaneMethanesulfonaMide, N-Methyl-4-(Methyl-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMino)-, trans-;N-methyl-1-((1r,4r)-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide;N-Methyl-1-(trans-4-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclohexyl)methanesulfonamide;Oclacitinib | | CAS: | 1208319-26-9 | | MF: | C15H23N5O2S | | MW: | 337.44 | | EINECS: | 950-980-7 | | Product Categories: | Inhibitors | | Mol File: | 1208319-26-9.mol |  |
| | Oclacitinib Chemical Properties |
| Melting point | 226-228°C | | density | 1.316±0.06 g/cm3(Predicted) | | vapor pressure | 0Pa at 20-25℃ | | storage temp. | Refrigerator, Under inert atmosphere | | solubility | DMSO (Slightly), Methanol (Slightly, Sonicated) | | pka | 11.59±0.40(Predicted) | | form | Solid | | color | Off-White to Pale Beige | | InChI | InChI=1S/C15H23N5O2S/c1-16-23(21,22)9-11-3-5-12(6-4-11)20(2)15-13-7-8-17-14(13)18-10-19-15/h7-8,10-12,16H,3-6,9H2,1-2H3,(H,17,18,19)/t11-,12- | | InChIKey | HJWLJNBZVZDLAQ-HAQNSBGRSA-N | | SMILES | [C@@H]1(CS(NC)(=O)=O)CC[C@@H](N(C)C2N=CN=C3NC=CC3=2)CC1 | | LogP | 1.38 at 35℃ and pH7 |
| | Oclacitinib Usage And Synthesis |
| Description | Oclacitinib is an oral JAK inhibitor that is a drug approved by the U.S. Food and Drug Administration (FDA) for use in canine atopic dermatitis (AD). The U.S. FDA and the European Medical Association have approved a number of JAK inhibitors, including baricitinib, ruxolitinib, federatinib, tofacitinib, upadacitinib, oclacitinib, but some of these drugs are still being studied. Oclacitinib mainly shows activity against JAK1-dependent cytokines and also inhibits the function of JAK2-dependent cytokines. oclacitinib modifies the production of cytokines such as IL-4 and IL-13, which are crucial for B-cell proliferation and maturation in the pathogenesis of pemphigus foliaceus. Oclacitinib could interdict the effects of IL-6, a cytokine involved in the Toll-like receptor 4-originated signaling pathway in the bladder epithelial cells, and IL-8, which could theoretically contribute to a decreased defense against the urinary pathogens[1-4]. | | Uses | Oclacitinib is a novel Janus kinase (JAK) inhibitor with activity against cytokines involved in allergy. | | Biological Activity | janus kinase (jak) enzymes are involved in cell signaling pathways activated by cytokines dysregulated in allergy. pf-03394197 (oclacitinib) is a novel janus kinase inhibitor. | | in vitro | pf-03394197 inhibited jak family members by 50% at concentrations ranging from 10 to 99 nm and did not inhibit a panel of 38 non-jak kinases. pf-03394197 was most potent at inhibiting jak1. pf-03394197 also inhibited the function of jak1-dependent cytokines involved in allergy and inflammation as well as pruritus. pf-03394197 had minimal effects on cytokines which did not activate the jak1 enzyme in cells [1]. | | in vivo | pf-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily was safe and efficacious in controlling the pruritus associated with allergic dermatitis. pf-03394197 provided itch relief within 24 h that persisted through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7 [2]. | | IC 50 | 10 nm for jak1 | | References | [1] Xin P, et al. The role of JAK/STAT signaling pathway and its inhibitors in diseases. International Immunopharmacology, 2020; 80: 549-56.
[2] Kalantari Y, et al. A literature review on Janus kinase (JAK) inhibitors for the treatment of immunobullous disorders. International Immunopharmacology, 2022; 110: 108923.[3] Erickson S, et al. New and emerging treatments for inflammatory itch. Annals of Allergy, Asthma Immunology, 2020; 126: 13-20.
[4] Xu P, et al. Janus kinases (JAKs): The efficient therapeutic targets for autoimmune diseases and myeloproliferative disorders. European Journal of Medicinal Chemistry, 2020; 129: 112155. |
| | Oclacitinib Preparation Products And Raw materials |
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