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Baricitinib

CAS No. : 1187594-09-7

產品活性：Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC₅₀s of 5.9 nM and 5.7 nM, respectively.

研究領域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶點：JAK

In Vitro: In cell-based assays, Baricitinib (INCB028050) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC₅₀ values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC₅₀=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC₅₀ value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM.

In Vivo: Baricitinib (INCB028050) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8⁺NKG2D⁺ cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice.

相關產品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  FDA-Approved Drug Library  |  Antiviral Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Drug-Induced Liver Injury (DILI) Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Anti-Liver Cancer Compound Library   |  Rare Diseases Drug Library  |  Children’s Drug Library  |  EMA-Approved Drug Library  |  Human Metabolite Library  |  Anti-Prostate Cancer Compound Library  |  Non-steroidal Anti-Inflammatory Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Pain-Related Compound Library  |  Withdrawn Drug Compound Library  |  JAK-IN-20  |  JAK1-IN-9  |  AT9283  |  RO495  |  TK4b  |  JAK-IN-17  |  (E/Z)-Zotiraciclib  |  JAK-IN-10  |  (3R,4S)-Tofacitinib  |  JAK3/BTK-IN-6  |  Tyk2-IN-5  |  Brevilin A  |  Broussonin E  |  Itacnosertib  |  RO8191  |  Axltide  |  Fosifidancitinib  |  JAK3-IN-6  |  Upadacitinib  |  JAK-IN-24  |  AZD-1480  |  Baricitinib-d₃  |  Tofacitinib-¹³C₃  |  AZ-3  |  Delphinidin chloride  |  TK4g  |  Tofacitinib Prodrug-1

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