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Purity: ≥98%
Baricitinib phosphate, the phosphate salt of Baricitinib which is also known as LY3009104 or INCB028050 or trade name Olumiant, is a potent, selective, ATP competitive and orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2. It is an FDA approved drug for the treatment of rheumatoid arthritis (RA) in the United States. In vitro, it is able to inhibit JAK1 and JAK2 with IC50 values in the low nanomolar range of 5.9 and 5.7 nM, respectively, while it displays low inhibitory activity for JAK3 and moderate activity for TYK2. Baricitinib inhibits intracellular signaling of several proinflammatory cytokines such as IL-6 and IL-23 at concentrations<50 nM. JAK signaling is central to a number of fundamental processes including the generation of RBCs. On Nov 20, 2020, the U.S. Food and Drug Administration also issued an emergency use authorization (EUA) for baricitinib to be used in combination with remdesivir, for the treatment of suspected or laboratory confirmed COVID-19 in hospitalized adults and pediatric patients two years of age or older requiring supplemental oxygen, invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO). On June 13, 2022, Olumiant (baricitinib) was approved by FDA to treat adult patients with severe alopecia areata, a disorder that often appears as patchy baldness and affects more than 300,000 people in the U.S. each year. Today’s action marks the first FDA approval of a systemic treatment (i.e. treats the entire body rather than a specific location) for alopecia areata.
| ln Vitro |
Baricitinib phosphate (INCB028050 phosphate) is a strong inhibitor of JAK signaling and function in experiments conducted on cells. Baricitinib has IC50 values of 44 nM and 40 nM, respectively, which prevent IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and the subsequent generation of the chemokine MCP-1 in PBMCs. INCB028050 also suppresses pSTAT3 activated by IL-23 (IC50=20 nM) in isolated naive T-cells. Significantly, at an IC50 value of 50 nM, this inhibition stopped the production of two pathogenic cytokines (IL-17 and IL-22) by Th17 cells, a subset of helper T cells with observable inflammatory and pathogenic characteristics. On the other hand, when evaluated at concentrations up to 10 μM, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 have no discernible effect in any of these assay systems[1].
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| ln Vivo |
Treatment with baricitinib phosphate (INCB028050 phosphate) suppresses the rise in hind paw volumes during the first two weeks of treatment by 50% at a dose of 1 mg/kg and by more than 95% at doses of 3 or 10 mg/kg when compared to the vehicle. It is feasible for animals exhibiting a noticeable improvement in swelling to have >100% inhibition because baseline paw volume measurements are obtained on treatment day 0 in animals with substantial symptoms of disease[1]. When compared to mice given with vehicle control, mice treated with baricitinib (0.7 mg/day) show significantly less inflammation as measured by H&E staining, less CD8 infiltration, and less MHC class I and class II expression. When compared to mice treated with a vehicle control, the number of CD8+NKG2D+ cells, which are important disease effectors in alopecia areata (AA) in humans and animals, is significantly reduced in mice treated with baricitinib[2].
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| 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 |
| Molecular Formula |
C16H20N7O6PS
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|---|---|
| Molecular Weight |
469.41
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| CAS # |
1187595-84-1
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| Related CAS # |
Baricitinib;1187594-09-7
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| SMILES |
S(C([H])([H])C([H])([H])[H])(N1C([H])([H])C(C([H])([H])C#N)(C1([H])[H])N1C([H])=C(C2=C3C([H])=C([H])N([H])C3=NC([H])=N2)C([H])=N1)(=O)=O.P(=O)(O[H])(O[H])O[H]
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| InChi Key |
FBPOWTFFUBBKBB-UHFFFAOYSA-N
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| Chemical Name |
(1-(Ethylsulfonyl)-3-(4-(7H-pyrrolo(2,3-d)pyrimidin-4-yl)-1H-pyrazol-1-yl)azetidin-3-yl)ethanenitrile phosphate
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| Synonyms |
trade name Olumiant; LY3009104 phosphate; LY-3009104; LY 3009104; INCB028050 phosphate; INCB-028050; INCB 028050; Baricitinib phosphate.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% CMC+0.25% Tween 80:30mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1303 mL | 10.6517 mL | 21.3033 mL | |
| 5 mM | 0.4261 mL | 2.1303 mL | 4.2607 mL | |
| 10 mM | 0.2130 mL | 1.0652 mL | 2.1303 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01398475 | Completed Has Results | Drug: LY3009104 | Chronic Inflammatory Disorder Arthritis, Rheumatoid |
Eli Lilly and Company | July 2011 | Phase 1 |
| NCT05452564 | Recruiting | Drug: Baricitinib 2 MG Oral Tablet | Human Immunodeficiency Virus | William Tyor | May 18, 2023 | Phase 2 |
| NCT04640168 | Completed Has Results | Drug: Baricitinib Drug: Dexamethasone | Recurrent Glioma Refractory Glioma |
National Institute of Allergy and Infectious Diseases (NIAID) |
December 2, 2020 | Phase 3 |
Cellular activity of INCB028050.J Immunol.2010 May 1;184(9):5298-307. |
Anti-inflammatory and DMARD activity of once daily INCB028050 in rats with established disease in the adjuvant arthritis model.J Immunol.2010 May 1;184(9):5298-307. |
Suppression of delayed-type hypersensitivity by INCB028050.J Immunol.2010 May 1;184(9):5298-307. |
INCB028050 is efficacious and well tolerated independently of effects on humoral immunity.J Immunol.2010 May 1;184(9):5298-307. |
INCB028050 improves clinical and histologic signs of disease in the murine CIA model. |
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