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Upadacitinib

Cat. No. M6297
Upadacitinib Structure
Synonym:

ABT-494

Size Price Availability Quantity
5mg USD 550 In stock
10mg USD 800 In stock
50mg USD 2500 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: In biochemical assays, Upadacitinib is 74-fold more selective for JAK-1 than for JAK-2 (which is involved in erythropoiesis) and 58-fold more selective for JAK-1 than for JAK-3 (which is involved in immunosurveillance). The enhanced selectivity of Upadacitinib for JAK-1 over JAK-2 and JAK-3 may offer an improved benefit–risk profile in patients with RA range.

In vivo: AbbVie’s second JAK inhibitor in development Upadacitinib has been described as a second-generation inhibitor. Multiple-dose Phase I studies are completed in 2013. In phase I trials, Upadacitinib is found to be safe and well-tolerated up to multiple doses of 24 mg twice daily using the immediate release formulation. Upadacitinib exposure is dose proportional in the evaluated multiple dose.

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 380.37
Formula C17H19F3N6O
CAS Number 1310726-60-3
Purity >98%
Solubility 22 mg/mL in DMSO
Storage at -20°C
References

Assessment of effect of CYP3A inhibition, CYP induction, OATP1B inhibition, and high-fat meal on pharmacokinetics of the JAK1 inhibitor upadacitinib.
Mohamed MF, et al. Br J Clin Pharmacol. 2017 Oct;83(10):2242-2248. PMID: 28503781.

JAK inhibitors: A broadening approach in rheumatoid arthritis.
Lam S. Drugs Today. 2016 Aug;52(8):467-469. PMID: 27722215.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Upadacitinib, ABT-494 supplier, JAK, inhibitors

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