Baricitinib

 CAS No.: 1187594-09-7  Cat No.: BP-300179  Purity: >98%  HPLC   HNMR   MS 4.5  

Baricitinib is a selective and orally bioactive inhibitor of JAK1 and JAK2. It has been approved by FDA for the treatment of rheumatoid arthritis (RA).

Baricitinib

Structure of 1187594-09-7

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Ligand for Target Protein
Molecular Formula
C16H17N7O2S
Molecular Weight
371.419
Appearance
White to Off-white Solid

* For research and manufacturing use only. Not for human or clinical use.

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1 g $199 In stock

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Popular Publications Citing BOC Sciences Products
Purity
>98%
Appearance
White to Off-white Solid
Application
the treatment of rheumatoid arthritis (RA)
Synonyms
LY3009104; 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile; Olumiant
Boiling Point
707.2±70.0 °C at 760 mmHg
Melting Point
212-215°C
Density
1.6±0.1 g/cm3
InChI Key
XUZMWHLSFXCVMG-UHFFFAOYSA-N
InChI
InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
Canonical SMILES
CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
1.Safety and efficacy of baricitinib at 24 weeks in patients with rheumatoid arthritis who have had an inadequate response to methotrexate.
Keystone EC1, Taylor PC2, Drescher E3, Schlichting DE4, Beattie SD4, Berclaz PY4, Lee CH4, Fidelus-Gort RK5, Luchi ME5, Rooney TP4, Macias WL4, Genovese MC6. Ann Rheum Dis. 2015 Feb;74(2):333-40. doi: 10.1136/annrheumdis-2014-206478. Epub 2014 Nov 27.
OBJECTIVES: To investigate baricitinib (LY3009104, formerly INCB028050), a novel, oral inhibitor of JAK1/JAK2 in patients with moderate to severe rheumatoid arthritis (RA) despite treatment with methotrexate.
2.Baricitinib in Patients with Refractory Rheumatoid Arthritis.
Genovese MC1, Kremer J1, Zamani O1, Ludivico C1, Krogulec M1, Xie L1, Beattie SD1, Koch AE1, Cardillo TE1, Rooney TP1, Macias WL1, de Bono S1, Schlichting DE1, Smolen JS1. N Engl J Med. 2016 Mar 31;374(13):1243-52. doi: 10.1056/NEJMoa1507247.
BACKGROUND: In phase 2 studies, baricitinib, an oral Janus kinase 1 and 2 inhibitor, reduced disease activity in patients with rheumatoid arthritis who had not previously received treatment with biologic disease-modifying antirheumatic drugs (DMARDs).
3.Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib.
Jabbari A1, Dai Z1, Xing L2, Cerise JE1, Ramot Y3, Berkun Y4, Sanchez GA5, Goldbach-Mansky R5, Christiano AM6, Clynes R7, Zlotogorski A3. EBioMedicine. 2015 Feb 26;2(4):351-5. doi: 10.1016/j.ebiom.2015.02.015. eCollection 2015.
BACKGROUND: Alopecia areata (AA) is an autoimmune disease resulting in hair loss with devastating psychosocial consequences. Despite its high prevalence, there are no FDA-approved treatments for AA. Prior studies have identified a prominent interferon signature in AA, which signals through JAK molecules.
ConcentrationVolumeMass1 mg5 mg10 mg
1 mM2.6924 mL13.4618 mL26.9237 mL
5 mM0.5385 mL2.6924 mL5.3847 mL
10 mM0.2692 mL1.3462 mL2.6924 mL
50 mM0.0538 mL0.2692 mL0.5385 mL

Dear sir. Can Baricitinib cross the blood-brain barrier in mice?

Yeah! Within a mouse model of HIV-associated neurocognitive impairment (HAND), Baricitinib crossed the blood-brain barrier and significantly reduced HIV-induced neuroinflammation marked by glial activation.

19/2/2016

Can Baricitinib inhibit allergen-induced airway eosinophilia in a mouse model?

Yes. In a mouse model of acute house dust mite-induced airway inflammation in BALB/c mice, Baricitinib effectively induced apoptosis and inhibited eosinophil chemotaxis and respiratory burst.

6/3/2018

Good afternoon, what is the biological activity of Baricitinib? Thanks.

Baricitinib preferentially inhibits JAK1 and JAK2 in a low nanomolar range, which in turn reduces the signaling of a variety of cytokines and growth factors.

22/7/2022

block the phosphorylation of STAT3

We treated the isolated T cells with Baricitinib to significantly inhibit IL-23-stimulated pSTAT3 and inhibit the production of two pathogenic cytokines (IL-17 and IL-22) by Th17 cells (helper T cell subtypes with obvious inflammatory and pathogenic characteristics).

9/2/2022

reduce the inflammation response

Our H&E staining and immunohistochemistry experiments showed that the Baricitinib-treated arthritis mouse model exhibited significantly reduced inflammation, reduced CD8 infiltration, and reduced MHC class I and II expression.

9/2/2022

inhibit pulmonary fibrosis

By immunohistochemistry, Western blot and MTT assay, we observed that Baricitinib inhibited the proliferation and migration of lung fibroblasts by inhibiting TGF-β1 signaling pathway, and finally effectively attenuated bleomycin (BLM) -induced pulmonary fibrosis in mice.

9/2/2022

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