Free shipping on all orders over $ 500

Upadacitinib

Cat. No. M6297
Upadacitinib Structure
Synonym:

ABT-494

Size Price Availability Quantity
5mg USD 495  USD550 In stock
10mg USD 720  USD800 In stock
50mg USD 2250  USD2500 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

Related JAK Products
Delphinidin chloride

Delphinidin (chloride) is an anthocyanidin, a natural plant pigment which can modulate JAK/STAT3 and MAPKinase signaling to induce apoptosis in HCT116 cells.

AZD4205

AZD4205 is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM.

PF-06826647

PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM.

PF-06700841 tosylate

PF-06700841 (Brepocitinib) tosylate is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively.

JAK3-IN-6 (Compound 2)

JAK3-IN-6 (Compound 2) CAS#: 1443235-95-7 is a potent and highly selective JAK3 inhibitor, with an IC50 of 0.15 nM.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.