2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. GLPG3667

GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases.

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GLPG3667 Chemical Structure

GLPG3667 Chemical Structure

CAS No. : 2308520-97-8

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Based on 1 publication(s) in Google Scholar

GLPG3667 Related Antibodies

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Description

GLPG3667 is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. GLPG3667 inhibits IFNα/pSTAT1, and the IC50 values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. GLPG3667 has the potential for the study of inflammatory and autoimmune diseases[1].

IC50 & Target[1]

Tyk2

2.3 nM (IC50)

JAK1

38 nM (IC50)

JAK2

7.3 nM (IC50)

JAK3

374 nM (IC50)

In Vitro

GLPG3667 shows dose-dependent inhibition of IFNα-induced STAT1 phosphorylation, demonstrating its selectivity and potency against TYK2 in relevant assays (PBMC and whole blood). In human peripheral blood mononuclear cells (PBMCs), the IC50 values for JAK1/TYK2, JAK1/JAK3, and JAK2 are 70 nM, 1113 nM, and 1022 nM, respectively. Its potency is notably higher in the TYK2-dependent pathway compared to JAK1 and JAK2 pathways, confirming its selective TYK2 inhibition profile[1].

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

GLPG3667 Related Antibodies
Parmacokinetics
Species Dose Route Indicator value
Mice 1mg/kg i.v. CLunbound 0.82 (9.9)L/h/kg
Mice 5mg/kg p.o. F 45%
Mice 1mg/kg i.v. Vss 1.9L/kg
Mice 5mg/kg p.o. AUC0-inf 2744ng·h/mL
Mice 1mg/kg i.v. T1/2 1.6hr
Mice 5mg/kg p.o. Cmax 1570ng/mL
Mice 5mg/kg p.o. Tmax 1.5hr
In Vivo

GLPG3667 (3-30 mg/kg; oral administration, once daily (q.d.); for 5 days) reduces dermal ear inflammation in an IL-23-induced in vivo mouse model of psoriasis[1].

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

Animal Model: Female BALB/c mice (IL-23-induced psoriasis model)[1]
Dosage: 3, 10, and 30 mg/kg (Solutol HS15/methyl cellulose 0.5% (2/98; v/v))
Administration: Oral administration, once daily (q.d.); for 5 days
Result: Successfully reduced ear pinna thickening and STAT3 phosphorylation in the epidermis and dermis. Additionally, reduced neutrophil infiltration in the dermis. However, there was no clear dose-response relationship observed, likely due to other pathways not impacted by TYK2 inhibition.
Molecular Weight

443.46

Formula

C22H21N9O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=NC=C(C(C)=C1)OC2=CC(NC3=NN=C(N4CCOCC4)C=C3)=C(N=CN5C)C5=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (112.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2550 mL 11.2750 mL 22.5499 mL
5 mM 0.4510 mL 2.2550 mL 4.5100 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2550 mL 11.2750 mL 22.5499 mL 56.3749 mL
5 mM 0.4510 mL 2.2550 mL 4.5100 mL 11.2750 mL
10 mM 0.2255 mL 1.1275 mL 2.2550 mL 5.6375 mL
15 mM 0.1503 mL 0.7517 mL 1.5033 mL 3.7583 mL
20 mM 0.1127 mL 0.5637 mL 1.1275 mL 2.8187 mL
25 mM 0.0902 mL 0.4510 mL 0.9020 mL 2.2550 mL
30 mM 0.0752 mL 0.3758 mL 0.7517 mL 1.8792 mL
40 mM 0.0564 mL 0.2819 mL 0.5637 mL 1.4094 mL
50 mM 0.0451 mL 0.2255 mL 0.4510 mL 1.1275 mL
60 mM 0.0376 mL 0.1879 mL 0.3758 mL 0.9396 mL
80 mM 0.0282 mL 0.1409 mL 0.2819 mL 0.7047 mL
100 mM 0.0225 mL 0.1127 mL 0.2255 mL 0.5637 mL
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GLPG3667 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLPG36672308520-97-8GLPG 3667GLPG-3667JAKJanus kinaseinflammatory diseasesInhibitorinhibitorinhibit

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