Upadacitinib
Upadacitinib (ABT-494) is a potent and selective JAK1 inhibitor with celluar IC50 of 8 nM, biochemical IC50 of 40 nM; displays 74-fold and 50-fold selectivity over JAK2 and JAK3, respectively; a second-generation JAK inhibitor in development for rheumatoid arthritis.Rheumatoid Arthritis Phase 3 Clinical (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) :Upadacitinib (0.1-10 mg/kg; oral gavage; twice a day for 10 days) demonstrates efficacy in rat arthritis models.
Product Specifications
CAS Number
1310726-60-3
Product Name Alternative
ABT-494 | ABT494 | ABT 494
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 22 mg/mL
Smiles
CCC1CN (CC1C2=CN=C3N2C4=C (NC=C4) N=C3) C (=O) NCC (F) (F) F
Molecular Formula
C17H19F3N6O
Molecular Weight
380.3676
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1-Pyrrolidinecarboxamide, 3-ethyl-4- (3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl) -N- (2,2,2-trifluoroethyl) -, (3S,4R) -
Available Sizes
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