Baricitinib (formerly INCB28050, LY3009104) is a selective orally bioavailable JAK1/JAK2 inhibitor. Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. INCB-28050 (baricitinib) inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 at concentrations <50 nM. Baricitinib also inhibits pSTAT3 stimulated by IL-23 with IC50 of 20 nM in isolated naive T-cells. Baricitinib (INCB028050) was also effective in multiple murine models of arthritis, with no evidence of suppression of humoral immunity or adverse hematologic effects. Baricitinib reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. INCB28050 (Baricitinib) (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 70 mg/mL|
Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.
Fridman JS, et al. J Immunol. 2010 May 1;184(9):5298-307. PMID: 20363976.
|Related JAK Products|
WHI-P97 is a JAK3 inhibitor with an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays.
SAR-20347 is a potent dual inhibitor of JAK1 and TYK2 with IC50 values of 23 and 0.6 nM, respectively.
Itacitinib, also known as INCB39110 or INCB039110, is a potent JAK1 tyrosine kinase inhibitor.
Solcitinib is a selective Janus kinase 1 (JAK1) inhibitor, for the treatment of psoriasis, lupus, and ulcerative colitis. Targer: JAK1
PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.