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产品价格:电议      采购度:1595      原产地:美洲
发布时间:2021/7/24 4:42:43 所属地区:上海 上海市
简要描述:
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) 是一种选择性的,可口服的 JAK1/JAK2 抑制剂,IC50 值分别为 nM 和 nM。
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CAS No. : 1187595-84-1
MCE 站:Baricitinib phosphate
产品活性:Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) 是一种选择性的,可口服的 JAK1/JAK2 抑制剂,IC50 值分别为 5.9 nM 和 5.7 nM。
研究领域:Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling
作用靶点:JAK
In Vitro: In cell-based assays, Baricitinib phosphate (INCB028050 phosphate) 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 phosphate (INCB028050 phosphate) 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.
相关产品: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 | Stem Cell Signaling Compound Library | FDA-Approved Drug 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-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | AG490 | Upadacitinib | AT9283 | Gandotinib | Lestaurtinib | Cucurbitacin I | Oclacitinib maleate | JANEX-1 | XL019 | Atractylenolide I | FLLL32 | LFM-A13 | Brevilin A | ZM39923 hydrochloride | Ginsenoside Rk1 | WHI-P154 | Curculigoside | FM-381 | RO8191 | Reticuline | TCS 21311 | WHI-P97 | Coumermycin A1 | Delphinidin chloride | Ilginatinib maleate | Protosappanin A | Dehydrocrenatidine | FM-479 | NSC 33994
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更新时间:2024/1/2 10:14:41
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