Home Tools
Log in
Cart

Delgocitinib

Catalog No. T15096   CAS 1263774-59-9
Synonyms: Corectim(Delgocitinib), JTE-052

Delgocitinib is a potent and specific JAK inhibitor with an IC50 value of 2.8, 2.6, 13 and 58 nM against JAK1, JAK2, JAK3 and Tyk2. Delgocitinib is involved in a variety of inflammatory and autoimmune diseases through JAK-dependent cytokines and can be widely used in the treatment of various inflammatory diseases. Delgocitinib is the world's first JAK topical compound for the treatment of atopic dermatitis.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Delgocitinib, CAS 1263774-59-9
Please contact us for prices and availability for the specification of product you are interested at.
Product consultation
Get quote
Purity: 98%
Contact us for more batch information
Biological Description
Chemical Properties
Storage & Solubility Information
Description Delgocitinib is a potent and specific JAK inhibitor with an IC50 value of 2.8, 2.6, 13 and 58 nM against JAK1, JAK2, JAK3 and Tyk2. Delgocitinib is involved in a variety of inflammatory and autoimmune diseases through JAK-dependent cytokines and can be widely used in the treatment of various inflammatory diseases. Delgocitinib is the world's first JAK topical compound for the treatment of atopic dermatitis.
Targets&IC50 Tyk2:58 nM, JAK1:2.8 nM, JAK2:2.6 nM, JAK3:13 nM
In vitro Delgocitinib inhibits the phosphorylation of Stat proteins induced by IL-2, IL-6, IL-23, GM-CSF, and IFN-α (IC50: 40±9, 33±14, 84±11, 304±22 and 18±3 nM, respectively), in these cell-based cytokine signaling assays and it also inhibits IL-2-induced proliferation of T cells in a concentration-dependent manner (IC50: 8.9±3.6 nM). Its potency is similar to that of tofacitinib (IC50:16 nM). Delgocitinib effectively inhibits all of the JAK subtypes ( IC50: 2.8±0.6, 2.6±0.2, 13±0 and 58±9 nM for JAK1, JAK2, JAK3 and Tyk2, respectively), in the enzymatic assays. Lineweaver-Burk plots display that the inhibition mode of Delgocitinib toward all JAKs is competitive with ATP (Ki: 2.1±0.3, 1.7±0.0, 5.5±0.3 and 14±1 nM for JAK1, JAK2, JAK3 and Tyk2, respectively) [1].
In vivo Delgocitinib inhibits radiographic and histological changes of bone destruction and cartilage destruction. Delgocitinib induces the IFN-γ production, however, the potency of the 1-h prior administration(ED50: 0.24 mg/kg) is higher than that of the 6-h prior administration (ED50: 1.3 mg/kg). In the administration from day 1, Delgocitinib prevents the development of hind paw swelling and histological changes of inflammatory cell infiltration and synovial cell hyperplasia. In the administration from day 15, Delgocitinib decreases the paw swelling in a dose-dependent manner. Delgocitinib ameliorates the inflammatory cell infiltration, synovial cell hyperplasia, and cartilage/bone destructions in the histological and radiographic examinations at the end of the study[1].
Synonyms Corectim(Delgocitinib), JTE-052
Molecular Weight 310.35
Formula C16H18N6O
CAS No. 1263774-59-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 50 mg/mL (161.11 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Tanimoto A, et al. Pharmacological properties of JTE-052: a novel potent JAK inhibitor that suppresses various inflammatory responses in vitro and in vivo. Inflamm Res. 2015 Jan;64(1):41-5

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below
Dosage
mg/kg
Average weight of animals
g
Dosing volume per animal
ul
Number of animals
Step Two: Enter the in vivo formulation
% DMSO
%
% Tween 80
% ddH2O
Calculate Reset

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculation
Molecular Weight Calculator
=
X
X

Molarity Calculator allows you to calculate the

  • Mass of a compound required to prepare a solution of known volume and concentration
  • Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Concentration of a solution resulting from a known mass of compound in a specific volume
See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

X
=
X

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

=
/

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

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.

Keywords

Delgocitinib 1263774-59-9 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors JAK Tyrosine Kinases Corectim(Delgocitinib) JTE052 Inhibitor Janus kinase inhibit JTE 052 JTE-052 inhibitor