Baricitinib

Key Product Details

Product Description

Baricitinib is a highly potent JAK1 and JAK2 inhibitor (IC₅₀ values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC₅₀ = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC₅₀ = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (K_d values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.

Product Specifications for Baricitinib

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Baricitinib

The following data is based on the product molecular weight 371.42.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.69 mL	13.46 mL	26.92 mL
5 mM	0.54 mL	2.69 mL	5.38 mL
10 mM	0.27 mL	1.35 mL	2.69 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 7 publications citing the usage of this product.

• Sorrell Family-wide structural analysis of human numb-associated protein kinases. Structure. 2016 PMID: 26853940
• Richardson Baricitinib as potential treatment for 2019-nCoV acute respiratory disease. Lancet. 2020 PMID: 32032529
• Fridman Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J.Immunol. 2010 PMID: 20363976

Product Documents for Baricitinib