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Upadacitinib

Name: Upadacitinib
Brand: TargetMol
SKU: T7503
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: ABT-494) Copy Product Info

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Synonyms: ABT-494

Catalog No. T7503 Copy Product Info

Purity: 99.94%

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Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.

Cas No. 1310726-60-3

Pack Size	Price	USA Stock	Global Stock
2 mg	$53	In Stock	In Stock
5 mg	$86	In Stock	In Stock
10 mg	$125	In Stock	In Stock
25 mg	$220	In Stock	In Stock
50 mg	$307	In Stock	In Stock
100 mg	$433	In Stock	In Stock
200 mg	$662	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$39	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.94%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Upadacitinib (ABT-494) is a highly potent, selective, and orally active JAK1 inhibitor with an IC₅₀ of 43 nM; its selectivity for JAK1 is approximately 74 times that for JAK2. Upadacitinib is being investigated for the treatment of autoimmune diseases such as rheumatoid arthritis and ankylosing spondylitis.
Targets & IC50	JAK3:2.3 μM, Tyk2:4.7 μM, JAK1:43 nM, JAK2:200 nM
In vitro	Methods: RAW264.7 mouse macrophages were treated with a concentration gradient (3, 6, 9 μg/mL) of upadacitinib for 24 hours, followed by cell viability assessment using the CCK-8 assay. Results: No cytotoxicity was observed at the concentrations of upadacitinib used. [1] Methods: Human whole blood was stimulated with IL-6 and treated with a concentration gradient of upadacitinib for 10 minutes. pSTAT3 expression in CD14+ monocytes and CD3+ T cells was detected by flow cytometry. Results: Upadacitinib inhibited IL-6 signaling in whole blood, with IC50 values of 78 nM (monocytes) and 207 nM (T cells).[2]
In vivo	Methods: Mice were randomly assigned to groups and administered daily oral gavage Upadacitinib (3 mg/kg and 6 mg/kg), once daily. Positive control: dexamethasone 4 mg/kg) for 5 consecutive days. CLP surgery was performed 4 hours after the final dose. Samples were collected 6 hours post-surgery, and 7-day survival rates were observed. Results: Upadacitinib (6 mg/kg) significantly improved the 7-day survival rate in CLP mice, reduced intestinal histopathological damage, and decreased bacterial counts in peritoneal lavage fluid. [1] Methods: Female Lewis rats developed arthritis via intra-articular injection of Mycobacterium tuberculosis emulsion into the right hind paw pad. Upadacitinib (1, 3, 10 mg/kg) was administered orally twice daily from days 7–17 post-onset. Paw swelling was measured; μCT assessed bone volume and density; histopathology was evaluated. Results: Upadacitinib exhibited dose-dependent reduction in paw swelling and bone destruction. [2] Methods: Healthy volunteers received single oral doses of upa-tibin (1, 3, 12, 24, 36, 48 mg) or tofacitinib (5 mg). Blood samples were collected at 1, 6, and 12 hours post-dose. Whole blood was stimulated ex vivo to measure inhibition of STAT phosphorylation. Results: Upa-tibin 3 mg inhibited IL-6-induced pSTAT3 by approximately 50%. [2]
Synonyms	ABT-494

Chemical Properties

Molecular Weight	380.37
Formula	C₁₇H₁₉F₃N₆O
Cas No.	1310726-60-3
Smiles	CC[C@@H]1CN(C[C@@H]1c1cnc2cnc3[nH]ccc3n12)C(=O)NCC(F)(F)F
Relative Density.	1.56 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (144.6 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6290 mL	13.1451 mL	26.2902 mL	131.4510 mL
5 mM	0.5258 mL	2.6290 mL	5.2580 mL	26.2902 mL
10 mM	0.2629 mL	1.3145 mL	2.6290 mL	13.1451 mL
20 mM	0.1315 mL	0.6573 mL	1.3145 mL	6.5725 mL
50 mM	0.0526 mL	0.2629 mL	0.5258 mL	2.6290 mL
100 mM	0.0263 mL	0.1315 mL	0.2629 mL	1.3145 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc