What is Baricitinib?
Baricitinib powder is white-like or white crystalline powder, odorless and tasteless, slightly soluble in water, soluble in hot water, relatively stable at normal temperature, insoluble in ethanol or acetone, and soluble in sodium hydroxide test solution.
Baricitinib is a Janus kinase (JAK) inhibitor. JAKs is an intracellular enzyme, which can transmit the signals produced by the interaction of cytokines or growth factor receptors on the cell membrane, which can affect the cellular process of hematopoietic function and immune cell function.
| Product name | Baricitinib |
| CAS | 1187594-09-7 |
| Molecular formula | C16H17N7O2S |
| Molecular weight | 371.42 |
| EINECS Number | 691-421-4 |
| Storage condition | -20°C |
| Melting point | 212-215°C |
| Solubility | Soluble in DMSO (up to 30mg/ml) or DMF (up to 50mg/ml). |
| Appearance | White powder |
| Boiling point | 707.2±70.0 °C at 760 mmHg |
| Density | 1.56 |
What is the mechanism of Baricitinib?
Baricitinib is a selective inhibitor of JAK2 and JAK1, and has little effect on JanusKinase and jak3orTYK2. This kinase and its related signal transduction and transcription activator (JAK-STAT) are the main intracellular pathways to control the amplitude and duration of signal transduction between cytokines and type I and type II cytokine receptors. These receptors lack intrinsic enzyme activity signal transduction that can be mediated; Janus Kinase \ Signaling and transcription activators are phosphorylated by JAK enzyme, which leads 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 signal passes through JAK-STAT signaling pathway. Therefore, JAK1 and JAK2 inhibitors can target multiple RA-related cytokine pathways, thus reducing the activation and proliferation of key immune cells of inflammatory cells. Baricitinib powder has no effect on JAK3. JAK3 may be related to the common γ chain receptor. Common cytokines of γ chain include IL-15 and IL-21, which mainly regulate lymphocyte activation, function and proliferation.
Product Specification
| Item | Specification | Results |
| Appearance | White or off-white solid powder | Complies |
| Identification | By IR | Complies |
| By HPLC | Complies | |
| Solubility | Soluble in DMF, sparingly soluble in THF, slightly soluble in methanol and acetonitrile, very sightly soluble in ethanol and dichloromethane, insoluble in water | Complies |
| Polymorphic Form | Polymorphic form 1 | Complies |
| Melting Point | 211ºC~216ºC | 212.8ºC~214.9ºC |
| Water Content | ≤ 0.50% | 0.10% |
| Heavy Metals | ≤ 20ppm | Complies |
| Residue on Ignition | ≤ 0.20% | 0.09% |
| Related Substance | Any single impurity: ≤0.10% | 0.06% |
| Total Impurities: ≤1.00% | 0.16% | |
| Assay (on the anhydrous basis) | 98.0%~102.0% | 99.94% |
| Particle Size | D90: ≤100µm | Complies |
| Conclusion: | Conform with enterprise specification. | |
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Where is Baricitinib applied?
1.Baricitinib powder is used to treat moderate to severe active rheumatoid arthritis (RA) in adults. Patients who are intolerant of one or more antirheumatic drugs can be treated with this product, which can be treated with single drug or combined with methotrexate.
2. Used in the fields of scientific research and chemical reagents.
HTML5 atlas of Baricitinib
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Biological activity of Baricitinib:
| Describe | Baricitinib is a selective and oral inhibitor of JAK1 and JAK2 with IC50 of 5.9 nM and 5.7 nM, respectively. |
| Target spot |
JAK2:5.7 nM (IC50) JAK1:5.9 nM (IC50) Tyk2:53 nM (IC50) JAK3:560 nM (IC50) |
| In vitro study | Baricitinib(INCB028050) has been proved to be an effective inhibitor of JAK signal transduction and function in cell-based assays. In PBMC, Baricitinib inhibited the phosphorylation of STAT3(pSTAT3) stimulated by IL-6 and the subsequent production of MCP-1, with IC50 values of 44nM and 40nM, respectively. In the isolated naive T cells, INCB028050 also inhibited PSTAT 3 stimulated by IL-23 (IC50 = 20 nm). Importantly, this inhibition prevented Th17 cells from producing two pathogenic cytokines (IL-17 and IL-22)- a helper T cell subtype with obvious inflammatory and pathogenic characteristics-with an IC50 value of 50nM. In sharp contrast, JAK1/2 inhibitors INCB027753 and INCB029843, which are similar in structure but ineffective, have no significant influence in any of these determination systems when tested at concentrations as high as 10 μ m. |
| In vivo study | Compared with the carrier, the paw volume increased by 50% after the treatment with INCB028050 for 2 weeks. The dosage was 1 mg/kg, > 95%, and the dosage was 3 or 10mg/kg. Because the baseline paw volume was measured on the 0 th day of treatment of animals with significant signs of disease, it may have a > 100% inhibitory effect on swelling, indicating a significant improvement in swelling. Baricitinib(0.7mg/day) treated mice, as assessed by H&E staining, showed significantly reduced inflammation, decreased CD8 infiltration and decreased MHC class I and II expression. Compared with mice treated with vector control, CD8+NKG2D+cells in mice treated with Baricitinib are the key effectors of diseases in mice and human alopecia (AA), which are greatly reduced. |
| Kinase experiment | Homogeneous time-resolved fluorometry (JAK1,837-1142; JAK2,828-1132; JAK3,718-1124; Tyk2,873-1187) or full-length enzyme (cMET). And Chk2) and peptide substrate. Each enzyme reaction was carried out with or without the test compound (11-point dilution), JAK, cMET or Chk2 enzyme, 500 nm (100nM for CHK2) peptide, ATP (Km or 1mM specific for each kinase), and 2.0％DMSO was added to the assay buffer. The calculated IC 50 value is the compound concentration required to suppress 50% fluorescence signal. Additional kinase assays were performed at Cerep using standard conditions of 200nM. Enzymes tested include: Abl, Akt1, AurA, AUB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1. |
| Cell experiment | Human PBMC was isolated by leukocyte separation, and then Ficoll-Hypaque centrifugation was performed. In order to determine the MCP-1 production induced by IL-6, PBMC was inoculated into RPMI 1640+10% FCS with 3.3×10 5 cells per well in the presence or absence of various concentrations of INCB028050(1 nM, 10 nM, 100 nM). 1μM and 10μM). After pre-incubation with the compound at room temperature for 10 minutes, cells were stimulated by adding 10ng/mL of human recombinant IL-6 to each well. The cells were incubated at 37℃ and 5% CO 2 for 48 hours. The supernatant was harvested and the level of human MCP-1 was analyzed by ELISA. The ability of INCB028050 to inhibit IL-6-induced MCP-1 secretion was reported as the required concentration (IC50) for 50% inhibition. Cell-Titer Glo [1] was used to proliferate Ba/F3-TEL-JAK3 cells within 3 days. |
| Animal experiment | Rats: Female rats (n = 6 in each group) were given a dose of 10mg/kg Baricitinib, and were given 10mL/kg by oral forced feeding. The first three rats were bled at 0 (before administration), 2 hours, 8 hours and 24 hours, and the second three rats were bled at 1,4 and 12 hours after administration. EDTA is used as anticoagulant, and the sample is centrifuged to obtain plasma. Analytical methods for quantifying INCB028050 have been developed and used to analyze samples from toxicological studies. The method combines protein precipitation extraction with 10% methanol in acetonitrile and carries out LC/MS/MS analysis. This method uses 0.1mL research sample to prove that the linear determination range is 1-5000nM. Use Analyst 1.3.1 to process data. Using weighted linear regression (1/x2) to determine the standard curve from the peak area comparison concentration. C3H/HeJ transplantation recipient mouse model of mouse AA was used in these experiments. In short, the alopecia skin from C3H/HeJ mice with spontaneous alopecia was transplanted to C3H/HeJ mice aged 8-10 weeks without disease. At the time of transplantation, an osmotic pump was implanted, which administered about 0.7mg/day of Baricitinib or placebo. The osmotic pump shall be replaced once a month. Time-event survival analysis of interval censored data is carried out. Survival and interval packets in r are used to perform log-rank test. The hypothesis that the survival distribution is equal in (n = 10) Baricitinib-treated mice and (n = 10) placebo-treated mice was rejected at the 5% level, and the P value was 0.0035 by using Sun's score for accurate log-rank double-sample test. |
| References |
[1]. Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307. [2]. Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5. [3]. Khan IM, et al. Intermuscular and perimuscular fat expansion in obesity correlates with skeletal muscle T cell and macrophage infiltration and insulin resistance. Int J Obes (Lond). 2015 Nov;39(11):1607-18. |
What's the difference between Baricitinib and Tofacitinib?
Firstly, both Baricitinib powder and Tofacitinib powder are selective JAK inhibitors. JAK(Janus kinase) is one of the key enzymes that control various cytokine signaling pathways and is considered to play an important role in the pathogenesis of autoimmune diseases. These two products can block the signal transduction of cytokines by inhibiting the activity of JAK kinase, thus reducing the activation of inflammation-related cells and the occurrence of inflammatory reactions.
However, there are some differences in selectivity and specificity between Baricitinib and Tofacitinib. Baricitinib tends to inhibit JAK1 and JAK2, while Tofacitinib has high selectivity for four JAK kinases (JAK1, JAK2, JAK3 and TYK2). This difference makes Baricitinib have some unique advantages in the treatment of specific diseases.
In terms of side effects, the side effects of Baricitinib and Tofacitinib are basically similar, but there are some minor differences. It is particularly important to note that because both products inhibit the activity of the immune system, they may increase the risk of infection when used.
What are the precautions of Baricitinib powder?
1. Ensure that the patient is not suffering from tuberculosis or other infections before use.
2. You should not use this product if you are allergic to Baricitinib powder or have any kind of infection.
3. "Live vaccine" cannot be inoculated during use; The vaccine inoculated at this time may not have the expected effect, nor can it completely protect the patients from the harm of the disease.
4. Baricitinib will affect the immune system of the body and may be more susceptible to infection, even serious or fatal infection.
How and where to buy Baricitinib powder wholesale?
You can trust our order because we have a good record of selling legal educational drugs.
We conduct independent laboratory tests on all products and then sell them to our respected customers.
A variety of shipping methods for you to choose
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Shipping method |
Cargo weight requirements |
Advantage |
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3-7 days |
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Suitable for under 50kg. |
We have warehouses in Germany and California, USA, |
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By Air |
Suitable for more than 50kg. |
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15-60 days |
By Sea |
Suitable for more than 500kg. |
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Note: This compound should be used for research purposes only. These claims have not been evaluated by the Food and Drug Administration. Please consult your doctor and learn about available studies before using them. This product is not intended to diagnose, treat, cure, or prevent any disease.
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