GLPG3667
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MedKoo CAT#: 556361

CAS#: 2308520-97-8

Description: GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation.

Chemical Structure

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GLPG3667
CAS# 2308520-97-8
Instruction

Theoretical Analysis

MedKoo Cat#: 556361
Name: GLPG3667
CAS#: 2308520-97-8
Chemical Formula: C22H21N9O2
Exact Mass: 443.18
Molecular Weight: 443.471
Elemental Analysis: C, 59.58; H, 4.77; N, 28.43; O, 7.22

Price and Availability

Size Price Availability Quantity
10mg USD 350 2 Weeks
25mg USD 550 2 Weeks
50mg USD 950 2 Weeks
100mg USD 1650 2 Weeks
1g USD 6950 2 Weeks
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Synonym: Tyk2-IN-14; GLPG3667; GLPG-3667; GLPG 3667;

IUPAC/Chemical Name: 4-methyl-5-((3-methyl-7-((6-morpholinopyridazin-3-yl)amino)-3H-imidazo[4,5-b]pyridin-5-yl)oxy)picolinonitrile

InChi Key: GXELZXDURVDKHP-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H21N9O2/c1-14-9-15(11-23)24-12-17(14)33-20-10-16(21-22(27-20)30(2)13-25-21)26-18-3-4-19(29-28-18)31-5-7-32-8-6-31/h3-4,9-10,12-13H,5-8H2,1-2H3,(H,26,27,28)

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

Appearance: To be determined

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 -4 C for short term (days to weeks) or -20 C for long term(months to years).

Solubility: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: The TYK2 inhibitor GLPG3667 demonstrated selectivity toward the three other JAK family members in several biochemical, cellular and human whole blood assays ex vivo and in vivo during a Phase 1 study (NCT04097938) in healthy HV. Pharmacological effects of GLPG3667 were demonstrated in a mouse model of psoriasis driven by IL-23 and in healthy HV challenged with IFNα. GLPG3667 is in development for the treatment of moderate to severe psoriasis.

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 443.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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https://acrabstracts.org/abstract/pharmacological-characterization-of-glpg3667-a-selective-tyk2-inhibitor-for-treatment-of-inflammatory-diseases/