1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK
  3. JAK1/TYK2-IN-3

JAK1/TYK2-IN-3 

Cat. No.: HY-143885
Handling Instructions

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.

For research use only. We do not sell to patients.

JAK1/TYK2-IN-3 Chemical Structure

JAK1/TYK2-IN-3 Chemical Structure

CAS No. : 2734918-37-5

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells[1].

IC50 & Target

Tyk2

6 nM (IC50)

JAK1

37 nM (IC50)

JAK2

140 nM (IC50)

JAK3

362 nM (IC50)

In Vitro

JAK1/TYK2-IN-3 (compound 48) (10, 20, 30 mg/kg) shows anti-inflammatory effect by regulating the formation of Th1, Th2, Th17 cells[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) inhibits the NF-κB signaling pathway by inhibits the JAK-STAT pathway, thereby reducing the inflammatory response in ulcerative colitis (UC) mice[1].
JAK1/TYK2-IN-3 (10, 20, 30 mg/kg) dose-dependently inhibits the mRNA expression of TNF-α, IL-1β, IL-12, IL-17A, IL-22, IFN-α, and IFN-β[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JAK1/TYK2-IN-3 (10, 20, 30 mg/kg; p.o.; twice a day for 12 days) shows a good therapeutic effect on ulcerative colitis (UC)[1].
JAK1/TYK2-IN-3 (5 mg/kg, p.o.) shows 23.7% oral bioavailability in rats[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-3 in male Sprague-Dawley rats[1].

compd dose(mg/kg) Administration Cmax(ng/mL) Cl (Lh-1kg-1) T1/2(h) AUC0-t(ng·h/mL) F (%)
48 5 mg/kg p.o. 400.4±55.3 11.3±5.2 2.4±2.1 440.9±157.0 23.7

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 weeks, 270-325g male Sprague-Dawley rats[1]
Dosage: 5 mg/kg
Administration: p.o.
Result: Showed 23.7% oral bioavailability in rats.
Animal Model: Six-eight week old male C57BL/6 mice, 20-22 g (2.5% dextran sulfate sodium (DSS)-induced acute UC mouse model)[1]
Dosage: 10, 20, 30 mg/kg
Administration: p.o., twice a day, 12 days
Result: Improved the infiltration of inflammatory factors and reduced the damage caused by DSS.
Molecular Weight

377.39

Formula

C17H21F2N7O

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JAK1/TYK2-IN-3
Cat. No.:
HY-143885
Quantity:
MCE Japan Authorized Agent: