Baricitinib
Baricitinib
CAS: 1187594-09-7
Molecular Formula: C16H17N7O2S
Baricitinib - Names and Identifiers
Baricitinib - Physico-chemical Properties
| Molecular Formula | C16H17N7O2S |
| Molar Mass | 371.42 |
| Density | 1.56 |
| Melting Point | 212-215°C |
| Solubility | Soluble in DMSO (74 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ |
| Appearance | solid |
| Color | White or off-white |
| pKa | 11.66±0.50(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20°C for up to 3 months. |
| Physical and Chemical Properties | White or white crystalline powder, odorless and tasteless, slightly soluble in water, dissolved in hot water, insoluble in ethanol or acetone, soluble in sodium hydroxide solution. Figure 2 shows barreotinib |
| Use | A selective inhibitor of JAK1 and JAK2. |
| In vitro study | In peripheral blood mononuclear cells Baricitinib inhibits the phosphorylation of IL-6-stimulated typical substrate STAT3 (pSTAT3) and the subsequent production of chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. Baricitinib also inhibited IL-23-stimulated phosphorylation of STAT3 in isolated naive T cells with an IC50 of 20 nM. |
| In vivo study | Baricitinib inhibits IL-6-stimulated STAT3 phosphorylation in whole blood with an IC50 of 128 nM. Baricitinib (10 mg/kg P. O.) is expected to inhibit JAK1/2 signaling (≥ 50% inhibition) for 8 H in rats. Baricitinib (10 mg/mL, P. O.) can suppress disease scores in the rat model of adjuvant arthritis and has a dose-dependent profile. Compared with the control group, 1 mg/kg Baricitinib treatment for two weeks can inhibit the growth of female deer paw volume by 50%,3 mg/kg or 10 mg/kg dose can inhibit more than 95%. Compared with the control group, 1 mg/kg Baricitinib treatment can inhibit the combined score of immune infiltration, edema, and the appearance of periarticular tissue in the adjuvant arthritis rat model by 27%,3 mg/kg can inhibit 64%,10 mg/kg can inhibit 82%. 1, 3 and 10 mg/kg Baricitinib reduced bone resorption in the adjuvant arthritis rat model by 15%, 61% and 67%, respectively. Baricitinib (10 mg/kg, once a day for 2 weeks, oral) can improve the normal structure and appearance of the ankle joint and tarsal bone in the adjuvant arthritis rat model. Baricitinib can reduce the phosphorylation level of STAT3 in the peripheral blood of Dalaya animals, and has dose-and time-dependent properties. Baricitinib (10 mg/mL, oral) increased the composite score of joint damage by 47% in a mouse model of collagen-induced arthritis (CIA). Baricitinib (10 mg/kg) reduced pannus (74%) and bone damage (78%) in a mouse model of collagen antibody-induced arthritis (CAIA), improvements in cartilage damage (43%) and inflammatory signaling (33%) resulted in a 53% improvement in the composite disease score. In the CIA and CAIA models, Baricitinib (10 mg/kg) inhibited delayed hypersensitivity by 48%. Baricitinib is effective in patients with active rheumatoid arthritis, while disease-modifying drugs and biologics are mostly ineffective. Baricitinib preferentially inhibited JAK1 and JAK2, with selectivity 10 times higher than Tyk2 and 100 times higher than JAK 3. The observed effect of GLPG-0634 on ACR20 is at least as good as that of tofacitinib and better than that of Baricitinib, because Baricitinib only moderately affected ACR20 values in a phase II clinical trial. Baricitinib has a dose-limiting side effect that induces anemia due to its effect on JAK2, but its efficacy is clear anyway. |
Baricitinib - Risk and Safety
| HS Code | 29350090 |
Baricitinib - Introduction
Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor. IC50 is 5.9 nM and 5.7 nM respectively, which is about 70 and 10 times higher than that of JAK3 and Tyk2, and has no inhibitory effect on c-Met and Chk2.
Last Update：2022-10-16 17:12:29
Baricitinib - Reference Information
| overview | baricotinib (Baricitinib) is an oral inhibitor of JAK kinase 1 and 2, commonly used in adults to treat moderate to severe active rheumatoid arthritis (RA). For patients with rheumatoid arthritis who have not used biological DMARDS drugs before, balectinib can reduce the activity of the disease. Figure 1 shows rheumatoid arthritis |
| mechanism of action | Baricitinib(olumiant) is a selective JAK2 and JAK1 inhibitor with little effect on Janus Kinase,jak3or TYK2. This kinase and its associated signal transducers and activators of transcription (JAK-STAT) are the main intracellular pathways that control the amplitude and duration of cytokine signaling with type I and type II cytokine receptors. These receptors lack the intrinsic enzyme activity signal transduction that can be mediated; Janus Kinase Signal Transducers and Activators of Transcription are phosphorylated by JAK enzyme, leading to STAT activation. Several inflammatory factors are involved in the pathogenesis of RA, including IL-6, granulocyte macrophage colony stimulating factor and (GM-CSF) factor. Interferon signaling passes through JAK-STAT signaling pathways. Therefore, JAK1 and JAK2 inhibitors can target multiple RA-related cytokine pathways, thereby reducing the activation and proliferation of key immune cells in inflammatory cells. Baricitinib has no effect on JAK3. JAK3 may be related to ordinary gamma chain receptors. Common γ-chain cytokines include IL-15 and IL-21, which mainly play a role in regulating lymphocyte activation, function and proliferation. |
| indications | 1. for the treatment of moderate to severe active rheumatoid arthritis (RA) in adults, patients with intolerance to one or more antirheumatic drugs can be treated with this product, which can be treated with monotherapy or combined with methotrexate. The curative effect of baricitinib on psoriasis, diabetic nephropathy, atopic dermatitis, systemic lupus erythematosus and other diseases is currently in phase II clinical stage. 2. Used in the field of scientific research and chemical reagents |
| usage and dosage | balectinib tablets: oral, once a day, the daily dose is 4mg. for patients over 75 years old and with a history of chronic recurrent infection, the daily dose of 2mg is recommended once a day. for patients treated with a daily dose of 4mg, if the condition has been continuously controlled, the daily dose can be changed to 2mg. |
| adverse reactions | the most common adverse reactions are headache, upper respiratory tract infection and nasopharyngitis. no opportunistic infection, tuberculosis infection and gastrointestinal perforation were found. |
| biological activity | Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor, IC50 is 5.9 nM and 5.7 nM respectively, which is about 70 and 10 times higher than that of JAK3 and Tyk2, and has no inhibitory effect on c-Met and Chk2. Phase 3. |
| Main reference | [1]http://www.qgyyzs.net/business/zr24393.htm. [2]http://china.guidechem.com/trade/pdetail9559647.html. [3] Huang Shijie. Barektinib significantly improves symptoms of moderate to severe rheumatoid arthritis [J]. International Journal of Pharmaceutical Research, 2016,43(04):785-786. [4]https://mp.weixin.qq.com/s?src=3×tamp=1513754264&ver=1&signature=i1sLq-BVKspZmlKilnWKYV66vP5IUXc336WNb0xIg3fKltMc6ie1y4uaq*9Fj1w2KkrtiMvPgAdSzJxOV13Z3ffA7GsWssD6qfGabEzB4Wwe-x0Zip-W62vTFyXlmYVLnOBkB0s3Jj9pNUEUKZ5ran9Ukf2GcH7Nk*fi4EA4IPg=. |
Last Update：2024-04-09 15:16:47
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