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Delgocitinib

Name: Delgocitinib
Brand: TargetMol
SKU: T15096
Price: 172 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: JTE-052, Corectim(Delgocitinib)) Copy Product Info

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Synonyms: JTE-052, Corectim(Delgocitinib)

Catalog No. T15096 Copy Product Info

Purity: 99.95%

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Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.

Cas No. 1263774-59-9

Pack Size	Price	USA Stock	Global Stock
1 mg	$172	In Stock	In Stock
5 mg	$328	In Stock	In Stock
10 mg	$513	In Stock	In Stock
25 mg	$977	In Stock	In Stock
50 mg	$1,490	In Stock	In Stock
100 mg	$2,170	In Stock	In Stock
200 mg	$2,920	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$367	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:99.95%

Appearance:Solid

Color:White

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COA HPLC HNMR LCMS

Product Introduction

Bioactivity

Description	Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.
Targets & IC50	JAK3:13 nM, TYK2:58 nM, JAK1:2.8 nM, JAK2:2.6 nM
In vitro	Methods: Enzymatic assays were performed to determine the inhibitory activity and mode of inhibition of Delgocitinib against JAK1, JAK2, JAK3, and Tyk2; cellular assays were conducted to examine the effects of Delgocitinib on cytokine-induced Stat protein phosphorylation and IL-2-induced T cell proliferation. Results: Delgocitinib potently inhibited JAK1, JAK2, JAK3, and Tyk2 in enzymatic assays with IC50 values of 2.8, 2.6, 13, and 58 nM, respectively, in an ATP-competitive manner (Ki values of 2.1, 1.7, 5.5, and 14 nM, respectively); in cellular assays, it concentration-dependently inhibited IL-2-, IL-6-, IL-23-, GM-CSF-, and IFN-α-induced Stat protein phosphorylation (IC50 values of 40, 33, 84, 304, and 18 nM, respectively) and suppressed IL-2-induced T cell proliferation (IC50 = 8.9 nM), with efficacy comparable to tofacitinib. [1]
In vivo	Methods: The in vivo anti-inflammatory and joint-protective effects of Delgocitinib were evaluated in an arthritis animal model. ED₅₀ was determined by single administration at different time points (1 h or 6 h before challenge); continuous administration was initiated from day 1 (prophylactic) or day 15 (therapeutic) to detect hind paw swelling, histopathological changes (inflammatory cell infiltration, synovial hyperplasia), and radiographic changes (cartilage/bone destruction). Results: Administration 1 h before challenge (ED₅₀=0.24 mg/kg) was more effective than 6 h before challenge (ED₅₀=1.3 mg/kg), and enhanced IFN-γ production. Administration from day 1 completely prevented paw swelling and histological lesions; administration from day 15 dose-dependently reduced swelling. Histological and X-ray examinations showed that Delgocitinib significantly improved inflammatory infiltration, synovial hyperplasia, and cartilage/bone destruction. [1] Methods: In a sclerodermatous chronic graft-versus-host disease mouse model (B10.D2 to BALB/c bone marrow transplantation), Delgocitinib ointment or eye drops (0.5%) were administered topically twice daily from day 7 to day 28 post-transplantation for 21 days, with control ointment or normal saline as the vehicle control. Results: Delgocitinib significantly reduced eyelid and skin inflammation and fibrosis, preserved meibomian gland area, and alleviated corneal epithelial damage. [2]
Synonyms	JTE-052, Corectim(Delgocitinib)

Chemical Properties

Molecular Weight	310.35
Formula	C₁₆H₁₈N₆O
Cas No.	1263774-59-9
Smiles	C[C@H]1CN(C(=O)CC#N)[C@]11CCN(C1)c1ncnc2[nH]ccc12
Relative Density.	1.41 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 240 mg/mL (773.32 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2222 mL	16.1108 mL	32.2217 mL	161.1084 mL
5 mM	0.6444 mL	3.2222 mL	6.4443 mL	32.2217 mL
10 mM	0.3222 mL	1.6111 mL	3.2222 mL	16.1108 mL
20 mM	0.1611 mL	0.8055 mL	1.6111 mL	8.0554 mL
50 mM	0.0644 mL	0.3222 mL	0.6444 mL	3.2222 mL
100 mM	0.0322 mL	0.1611 mL	0.3222 mL	1.6111 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.