Upadacitinib Research Grade Compound (JAK1 Inhibitor) Supplier — UPOR Biotech
Upadacitinib (ABT-494) — selective Janus kinase 1 (JAK1) inhibitor with IC50 43 nM and approximately 74-fold selectivity for JAK1 over JAK2. Blocks JAK1-dependent cytokine signaling (IL-6, IL-2, IFN-γ, IL-15) and the downstream JAK/STAT pathway — a cornerstone pharmacological tool for immunology and chronic inflammation research. CAS 1310726-60-3, C₁₇H₁₉F₃N₆O, MW 380.37 g/mol. Research Grade (RUO) reference standard — bulk supplier of analytical-grade JAK1 inhibitor research compound from UPOR Biotech.
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Upadacitinib (CAS 1310726-60-3, C₁₇H₁₉F₃N₆O, MW 380.37 g/mol) is a potent, orally active, selective Janus kinase 1 (JAK1) inhibitor belonging to the pyrrolidine-carboxamide small-molecule class, supplied as the single (3S,4R) enantiomer. It is the active pharmaceutical ingredient referenced in the commercial JAK inhibitor Rinvoq — provided here strictly as a Research Use Only (RUO) reference compound for non-clinical study. Mechanistically, upadacitinib achieves selective JAK1 inhibition with an IC50 of 43 nM, exhibiting approximately 74-fold selectivity for JAK1 over JAK2 in relevant cellular assays. This selectivity profile is biologically meaningful: JAK1 pairs with JAK2, JAK3, and TYK2 to transduce the majority of pro-inflammatory cytokine signals. By inhibiting JAK1, upadacitinib blocks JAK1-dependent cytokine signaling cascades — including the IL-6, IL-2, IFN-γ, and IL-15 receptor pathways — and suppresses downstream JAK1/STAT phosphorylation, providing a precise tool for interrogating the JAK-STAT axis in inflammation research.
As a leading supplier of research-grade pharmaceutical reference compounds, UPOR Biotech provides upadacitinib for the immunology and inflammation pharmacology community — supporting rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, and Crohn’s disease research models, as well as JAK/STAT signaling and cytokine biology studies. Research Use Only (RUO) — not for human diagnostic or therapeutic use. Each lot is manufactured under ISO 9001 and cGMP-compliant processes at an FDA-registered facility and released with a full Certificate of Analysis (COA) documenting ≥98% HPLC purity, heavy metals ≤10 ppm, and optical rotation of the single enantiomer. Available in 1/5/10/50 g analytical packaging with a 3-year shelf life and complete lot traceability.
Upadacitinib vs Tofacitinib — Selective JAK1 Inhibitor vs Pan-JAK Inhibitor
When comparing upadacitinib vs tofacitinib, the defining difference is kinase selectivity. Upadacitinib was engineered for JAK1 selectivity, achieving ~74-fold selectivity for JAK1 over JAK2 in cellular assays while retaining potent JAK1-dependent cytokine blockade. Tofacitinib, in contrast, is a broader pan-JAK inhibitor that inhibits JAK1, JAK2, JAK3, and TYK2 with less discrimination — particularly stronger JAK3 activity that can affect JAK3/STAT5-dependent homeostatic signaling. For researchers dissecting JAK1-specific contributions to inflammatory pathways, upadacitinib’s selectivity profile is a key differentiator in JAK-STAT pharmacology research, enabling cleaner attribution of phenotypic effects to JAK1-dependent signaling. Both are small-molecule JAK inhibitors; the selectivity index, not raw potency, governs experimental interpretation.
Technical Specifications
| Property | Specification |
|---|---|
| Product Name | Upadacitinib (ABT-494) — Research Grade (RUO) |
| Synonyms | Upadacitinib; ABT-494 |
| CAS Number | 1310726-60-3 |
| Molecular Formula | C₁₇H₁₉F₃N₆O |
| Molecular Weight | 380.37 g/mol |
| IUPAC Name | (3S,4R)-3-Ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide |
| Compound Class | Small-molecule selective JAK1 inhibitor (pyrrolidine-carboxamide) |
| Reference Brand | Rinvoq (research reference compound only — RUO) |
| Target / Kinase | JAK1 (Janus kinase 1) |
| Mechanism | Selective JAK1 inhibition (IC50 43 nM); blocks JAK1-dependent cytokine signaling (IL-6, IL-2, IFN-γ, IL-15) and JAK1/STAT pathway activation |
| Kinase Selectivity | ~74-fold selective for JAK1 over JAK2 (cellular assays) |
| Route of Administration (Reference) | Orally active in vivo reference; not for human administration (RUO) |
| Purity (HPLC) | ≥98.0% |
| Appearance | White to off-white solid |
| Melting Point | ~153–155°C |
| Solubility | DMSO ≥50 mg/mL |
| Optical Rotation | Single (3S,4R) enantiomer |
| Heavy Metals | ≤10 ppm |
| Water Content | ≤1.0% |
| Storage | 2–8°C, sealed, protected from light and moisture |
| Grade | Research Grade (RUO) |
| Applications | Immunology/inflammation research; JAK/STAT signaling; cytokine biology; analytical reference standard |
| Certifications | ISO 9001, cGMP, FDA facility registration |
| Packaging | 1/5/10/50 g |
| Shelf Life | 3 years |
| Disclaimer | Research Use Only (RUO) — not for human diagnostic or therapeutic use |
Key Benefits — Upadacitinib Research Grade
Potent Selective JAK1 Inhibition — IC50 43 nM
Upadacitinib delivers potent JAK1 inhibition at IC50 43 nM, directly suppressing JAK1-dependent cytokine signaling. This concentration of activity is ideal for dose-response pharmacology and pathway-engagement studies in immune and inflammation research models.
IC50 43 nM~74-Fold JAK1/JAK2 Selectivity — Engineered Selectivity Profile
Approximately 74-fold selectivity for JAK1 over JAK2 in cellular assays sets upadacitinib apart from broader inhibitors. This selectivity enables clean attribution of experimental effects to JAK1-dependent signaling, a critical advantage in JAK-STAT pharmacology research.
~74-fold JAK1/JAK2JAK/STAT & Cytokine-Signaling Blockade
Blocks JAK1-dependent cytokine cascades (IL-6, IL-2, IFN-γ, IL-15) and downstream JAK/STAT pathway phosphorylation. A validated molecular tool for dissecting the signaling networks that drive autoimmune and chronic inflammatory disease.
JAK/STAT Blockade≥98% HPLC Purity Reference Standard
≥98% HPLC purity with documented single (3S,4R) enantiomer, heavy metals ≤10 ppm, and full COA. Manufactured under ISO 9001 and cGMP-compliant processes — a reliable analytical reference standard for method development and method validation.
≥98% HPLCApplications
Rheumatoid Arthritis & Autoimmunity Research
Studying JAK1-dependent IL-6 and IFN-γ signaling in synovial inflammation, autoantibody-driven models, and disease-modifying immunomodulation. RUO reference only.
Psoriatic Arthritis & Atopic Dermatitis Studies
Investigating IL-2/IL-15 and type-1/type-2 cytokine crosstalk in skin and joint inflammatory models. Upadacitinib enables pathway-selective inhibition in dermatology-focused research.
Inflammatory Bowel Disease (UC/Crohn’s) Research
Modeling JAK/STAT-driven mucosal inflammation in ulcerative colitis and Crohn’s disease. Supports mechanism-of-action and cytokine-biology studies in gut immunology.
JAK/STAT Signaling Pathway Assays
Probing STAT phosphorylation, gene-transcription readouts, and JAK1-vs-JAK2 selectivity in cell-based assays. A precise reference inhibitor for pathway dissection.
Cytokine-Mediated Inflammation Models
Benchmarking IL-6, IL-2, IFN-γ, and IL-15 driven responses in macrophage, T-cell, and fibroblast models. Validated tool for anti-inflammatory pharmacology.
Analytical Reference Standard & Method Development
Certified reference material for HPLC method development, system suitability, and small-molecule API quantification in quality-control and bioanalytical laboratories.
Frequently Asked Questions
Upadacitinib (ABT-494) is a potent, orally active, selective JAK1 inhibitor with an IC50 of 43 nM. It blocks JAK1-dependent cytokine signaling (IL-6, IL-2, IFN-γ, IL-15) and suppresses downstream JAK/STAT pathway phosphorylation, reducing pro-inflammatory gene transcription. It exhibits ~74-fold selectivity for JAK1 over JAK2. As a Research Use Only (RUO) reference compound, it provides a precise pharmacological tool for studying JAK1-mediated inflammation and JAK-STAT signaling in cell-based and in vivo research models.
Upadacitinib was engineered for JAK1 selectivity (~74-fold over JAK2) while retaining potent JAK1-dependent cytokine blockade. Tofacitinib is a broader pan-JAK inhibitor targeting JAK1, JAK2, JAK3, and TYK2 with less discrimination. In JAK-STAT pharmacology research, the selectivity index is the key differentiator: upadacitinib enables cleaner attribution of effects to JAK1-dependent pathways, whereas tofacitinib’s broader coverage can complicate mechanistic interpretation.
Key applications include autoimmune and inflammatory disease research (rheumatoid arthritis, psoriatic arthritis, atopic dermatitis, ulcerative colitis, Crohn’s disease), JAK/STAT signaling pathway assays, cytokine biology studies, and use as an analytical reference standard for HPLC method development and small-molecule API qualification. Upadacitinib is also used in dose-response and selectivity profiling experiments that benchmark JAK1-selective pharmacology.
Store at 2–8°C, protected from light and moisture, in the sealed original container. Prepare DMSO stock solutions (≥50 mg/mL) under anhydrous conditions and aliquot to avoid repeated freeze-thaw cycles. Handle with appropriate PPE in a well-ventilated fume hood. As a Research Use Only (RUO) pharmaceutical reference compound, upadacitinib is not intended for human diagnostic or therapeutic use.
Every shipment includes a COA documenting ≥98% HPLC purity, heavy metals ≤10 ppm, optical rotation of the single (3S,4R) enantiomer, and residual solvents, plus an MSDS and lot-specific documentation. Production is ISO 9001 and cGMP compliant at an FDA-registered facility. All material is Research Grade (RUO) — for research use only, not for human diagnostic or therapeutic use.