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Baricitinib

Cat. No. M2039
Baricitinib Structure
Synonym:

INCB28050, LY3009104

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 85 In stock
50mg USD 260 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 371.42
Formula C16H17N7O2S
CAS Number 1187594-09-7
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Baricitinib, INCB28050, LY3009104 supplier, JAK, inhibitors

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