Baricitinib (LY3009104, INCB028050)
(Synonyms: 巴瑞替尼; LY3009104; INCB028050) 目录号 : GC14844
Baricitinib (LY3009104, INCB028050)是一种高效口服JAK1/JAK2抑制剂，对JAK1和JAK2的IC50值分别为5.9nM和5.7nM。
Cas No.:1187594-09-7
Sample solution is provided at 25 µL, 10mM.
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Baricitinib (LY3009104, INCB028050) is a potent orally active inhibitor of JAK1 and JAK2 with IC50 values of 5.9 and 5.7nM, respectively [1]. By inhibiting JAK1 and JAK2 enzymes, Baricitinib can block the signal transduction of a variety of cytokines related to COVID-19 immunopathology, and play an antiviral effect by targeting the host factors that viral invasion cells depend on and inhibiting the up-regulation of angiotensin-converting enzyme 2 (ACE2) driven by type I interferon[2]. Baricitinib has been widely used to regulate cytokine release and related signaling of leukocyte subsets as well as inflammatory responses[3].
In vitro, Baricitinib treatment for 24 hours significantly inhibited TGF-β1-induced proliferation of Mlg cells and NIH-3T3 cells, with IC50 values of 113.3 and 148.0μM, respectively[4]. Baricitinib treatment at 5µM for 24h significantly inhibited lipopolysaccharide (10µg/ml)-induced oxidative stress and inflammation in periodontal ligament stem cells (PDLSCs) and promoted osteogenic differentiation of the cells[5].
In vivo, Baricitinib treatment via oral administration (10mg/kg) twice daily for 8 weeks inhibited abnormal B cell activation and podocyte abnormalities and effectively attenuated autoimmune features, including renal inflammation, in lupus-prone mice[6]. Oral administration of Baricitinib at a dose of 10mg/kg/day for 16 weeks suppressed metabolic disorders and ameliorated muscle steatosis, mesangial expansion, and associated proteinuria in mice induced by a high-fat and high-sugar diet[7]. Oral administration of Baricitinib at a dose of 5mg/kg/day for a week can reduce myocardial cell widening, inflammatory infiltration, and fibrous tissue hyperplasia in isoproterenol (ISO)-induced myocardial fibrosis mice[8].
References:
[1] Fridman J S, Scherle P A, Collins R, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050[J]. The Journal of Immunology, 2010, 184(9): 5298-5307.
[2] Jorgensen S C J, Tse C L Y, Burry L, et al. Baricitinib: a review of pharmacology, safety, and emerging clinical experience in COVID‐19[J]. Pharmacotherapy: The Journal of Human Pharmacology and Drug Therapy, 2020, 40(8): 843-856.
[3] McInnes I B, Byers N L, Higgs R E, et al. Comparison of baricitinib, upadacitinib, and tofacitinib mediated regulation of cytokine signaling in human leukocyte subpopulations[J]. Arthritis research & therapy, 2019, 21(1): 183.
[4] Gu S, Liang J, Zhang J, et al. Baricitinib attenuates bleomycin-induced pulmonary fibrosis in mice by inhibiting TGF-β1 signaling pathway[J]. Molecules, 2023, 28(5): 2195.
[5] Yang P, Shi F, Zhang Y. Baricitinib alleviates lipopolysaccharide‑induced human periodontal ligament stem cell injury and promotes osteogenic differentiation by inhibiting JAK/STAT signaling[J]. Experimental and Therapeutic Medicine, 2022, 25(2): 74.
[6] Lee J, Park Y, Jang S G, et al. Baricitinib attenuates autoimmune phenotype and podocyte injury in a murine model of systemic lupus erythematosus[J]. Frontiers in Immunology, 2021, 12: 704526.
[7] Collotta D, Hull W, Mastrocola R, et al. Baricitinib counteracts metaflammation, thus protecting against diet-induced metabolic abnormalities in mice[J]. Molecular Metabolism, 2020, 39: 101009.
[8] Feng R, Liu H, Chen Y. Baricitinib represses the myocardial fibrosis via blocking JAK/STAT and TGF-β1 pathways in vivo and in vitro[J]. BMC Cardiovascular Disorders, 2025, 25(1): 65.
Baricitinib (LY3009104, INCB028050)是一种高效口服JAK1/JAK2抑制剂，对JAK1和JAK2的IC50值分别为5.9nM和5.7nM[1]。通过抑制JAK1/JAK2酶活性，Baricitinib可阻断多种COVID-19免疫病理相关细胞因子的信号转导，并通过靶向病毒入侵细胞的宿主依赖因子及抑制I型干扰素驱动的血管紧张素转换酶2(ACE2)上调发挥抗病毒作用[2]。Baricitinib已广泛应用于细胞因子释放、白细胞亚群相关信号及炎症反应的调控[3]。
在体外，Baricitinib处理24小时能显著抑制TGF-β1诱导的Mlg细胞和NIH-3T3细胞增殖，IC50值分别为113.3 μM和148.0 μM[4]。使用5µM的Baricitinib处理牙周膜干细胞(PDLSCs)24小时，可显著抑制脂多糖(10µg/ml)诱导的氧化应激与炎症反应，并促进细胞成骨分化[4]。
在体内，每日两次口服10 mg/kg剂量的Baricitinib连续8周，能抑制狼疮易感小鼠的异常B细胞活化及足细胞异常，有效减轻肾脏炎症等自身免疫特征[6]。每日口服10 mg/kg/day剂量的Baricitinib连续16周，可抑制高脂高糖饮食诱导的小鼠代谢紊乱，改善肌肉脂肪变性、系膜扩张及相关蛋白尿[7]。每日口服5mg/kg/day剂量的Baricitinib连续1周，能减轻异丙肾上腺素(ISO)诱导的心肌纤维化小鼠的心肌细胞肥大、炎症浸润及纤维组织增生[8]。
| Cell experiment [1]: | |
Cell lines | Human periodontal ligament stem cells |
Preparation Method | Human periodontal ligament stem cells (PDLSCs) were cultured in DMEM medium containing 10% fetal bovine serum (FBS) at 37℃ in an incubator with 5% CO2. 5×103 PDLSCs were seeded in 96-well plates and treated with lipopolysaccharide (10µg/ml) for 24h at 37℃ to mimic the inflammatory microenvironment of periodontitis. PDLSCs were treated with Baricitinib (1.0, 2.5, and 5.0µM) for 24h at 37℃ in the presence or absence of lipopolysaccharide, followed by the addition of CCK-8 reagent, and optical density values were recorded at a wavelength of 450nm. |
Reaction Conditions | 1.0, 2.5, and 5.0µM; 24h |
Applications | Baricitinib dose-dependently increased the viability of PDLSCs following lipopolysaccharide treatment. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Male C57BL/6 mice (6-8 weeks old, 20-25g) were housed in a standard environment. Mice were selected and administered a single intratracheal instillation of bleomycin (BLM) dissolved in normal saline (0.9% NaCl) via a high-pressure syringe to establish the mouse models of bleomycin-induced pulmonary fibrosis. A total of 28 mice were randomly divided into 4 groups, with 7 mice in each group: NaCl group, BLM group, positive control group (BLM+ Nintedanib, 100mg/kg/day), and BLM+ Baricitinib group (BLM+ Baricitinib, 40mg/kg/day). All treatment groups were treated by gavage. The drugs were suspended in double-distilled water, and an equal volume of solvent (double-distilled water) was added to the control and BLM groups. After 7 days of Baricitinib treatment, the mice were sacrificed, and the left lung was removed for pathological staining, and the right lung was used for hydroxyproline and fibrosis marker detection. |
Dosage form | 40mg/kg/day for 7 days; p.o. |
Applications | Baricitinib treatment significantly decreased the content of hydroxyproline and the area of fibrosis in the lungs of mice. |
References: | |
| Cas No. | 1187594-09-7 | SDF | |
| 别名 | 巴瑞替尼; LY3009104; INCB028050 | ||
| 化学名 | 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile | ||
| Canonical SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 | ||
| 分子式 | C16H17N7O2S | 分子量 | 371.42 |
| 溶解度 | ≥ 18.57 mg/mL in DMSO | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6924 mL | 13.4618 mL | 26.9237 mL |
| 5 mM | 538.5 μL | 2.6924 mL | 5.3847 mL |
| 10 mM | 269.2 μL | 1.3462 mL | 2.6924 mL |
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- Purity: >99.50%
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