Baricitinib

• CAT Number: I000674
• CAS Number: 1187594-09-7
• Molecular Formula: C₁₆H₁₇N₇O₂S
• Molecular Weight: 371.42
• Purity: ≥95%
• Target: JAK
• Solubility: DMSO: ≤ 25 mg/mL
• Storage: 3 years -20C powder
• IC50: JAK1 (5.9 nM) and JAK2 (5.7 nM) [1].
• 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)
• InChIKey: XUZMWHLSFXCVMG-UHFFFAOYSA-N
• SMILES: CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

Baricitinib (CAT: I000674) is a selective inhibitor of Janus kinase (JAK) enzymes, specifically targeting JAK1 and JAK2. It is primarily used in the treatment of inflammatory conditions, such as rheumatoid arthritis. Baricitinib works by blocking the activity of JAK enzymes, which play a crucial role in the signaling pathways involved in inflammation and immune response. By inhibiting JAK1 and JAK2, baricitinib helps to reduce inflammation and alleviate the symptoms associated with rheumatoid arthritis.

Reference

1:[Success for a new generation of disease-modifying antirheumatic drugs : The Janus kinase inhibitor baricitinib in rheumatoid arthritis]. Keyßer G.Z Rheumatol. 2017 Apr 26. doi: 10.1007/s00393-017-0307-3. [Epub ahead of print] Review. German. No abstract available. PMID: 28447156 2:Efficacy and safety of baricitinib in Japanese patients with active rheumatoid arthritis: A 52-week, randomized, single-blind, extension study. Tanaka Y, Ishii T, Cai Z, Schlichting D, Rooney T, Macias W.Mod Rheumatol. 2017 Apr 25:1-10. doi: 10.1080/14397595.2017.1307899. [Epub ahead of print] PMID: 28440680 3:Patient-reported outcomes from a phase III study of baricitinib in patients with conventional synthetic DMARD-refractory rheumatoid arthritis. Emery P, Blanco R, Maldonado Cocco J, Chen YC, Gaich CL, DeLozier AM, de Bono S, Liu J, Rooney T, Chang CH, Dougados M.RMD Open. 2017 Mar 21;3(1):e000410. doi: 10.1136/rmdopen-2016-000410. eCollection 2017. PMID: 28405473 Free PMC Article4:Questioning the Effectiveness of Baricitinib for Pulmonary Manifestations of Rheumatoid Arthritis. Chertoff J, Ataya A.Am J Respir Crit Care Med. 2017 Mar 30. doi: 10.1164/rccm.201703-0552LE. [Epub ahead of print] No abstract available. PMID: 28358994 5:Baricitinib: First Global Approval. Markham A.Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3. Review. PMID: 28290136 6:Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Kuriya B, Cohen MD, Keystone E.Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. Review. PMID: 28255337 Free PMC Article7:Rheumatoid Arthritis: Baricitinib more effective than adalimumab. McHugh J.Nat Rev Rheumatol. 2017 Apr;13(4):197. doi: 10.1038/nrrheum.2017.32. Epub 2017 Mar 2. No abstract available. PMID: 28250459 8:Baricitinib versus Placebo or Adalimumab in Rheumatoid Arthritis. Taylor PC, Keystone EC, van der Heijde D, Weinblatt ME, Del Carmen Morales L, Reyes Gonzaga J, Yakushin S, Ishii T, Emoto K, Beattie S, Arora V, Gaich C, Rooney T, Schlichting D, Macias WL, de Bono S, Tanaka Y.N Engl J Med. 2017 Feb 16;376(7):652-662. doi: 10.1056/NEJMoa1608345. PMID: 28199814 9:Comparative efficacy and safety of baricitinib 2 mg and 4 mg in patients with active rheumatoid arthritis : A Bayesian network meta-analysis of randomized controlled trials. Lee YH, Bae SC.Z Rheumatol. 2017 Jan 17. doi: 10.1007/s00393-016-0254-4. [Epub ahead of print] PMID: 28097393 10:Effects of Baricitinib on Lipid, Apolipoprotein, and Lipoprotein Particle Profiles in a Phase IIb Study of Patients With Active Rheumatoid Arthritis. Kremer JM, Genovese MC, Keystone E, Taylor PC, Zuckerman SH, Ruotolo G, Schlichting DE, Crotzer VL, Nantz E, Beattie SD, Macias WL.Arthritis Rheumatol. 2017 May;69(5):943-952. doi: 10.1002/art.40036. PMID: 28029752