GLPG0634 analogue

Alias: Filgotinib-analogue; GLPG-0634 analogue;Filgotinib analogue, GLPG0634 analog; GLPG 0634 analogue; GLPG 0634 analogue

Cat No.:V0328 Purity: ≥98%

COA Product Data Instructions for use SDS

GLPG0634 analogue, an analog ofFilgotinib (GLPG0634),is a novel, potent andselective Janus kinase-JAK1 inhibitor with potential anti-inflammatory activity.

GLPG0634 analogue Chemical Structure CAS No.: 1206101-20-3
Product category: JAK

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of GLPG0634 analogue:

Filgotinib (GLPG-0634)

Official Supplier of:

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

GLPG0634 analogue, an analog of Filgotinib (GLPG0634), is a novel, potent and selective Janus kinase-JAK1 inhibitor with potential anti-inflammatory activity. It inhibits JAK1, JAK2, JAK3, and TYK2 with IC50s of 10, 28, 810, and 116 nM, respectively. It has the potential to be used for treating RA-rheumatoid arthritis. It dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.

Biological Activity I Assay Protocols (From Reference)

ln Vitro

JAK-STAT and OSM/IL-lβ pathways are both inhibited by GLPG0634 analog (Compoun 176), with respective EC50 values ranging from 101 to 500 nM[1]. In both rats and humans, the GLPG0634 analog has microsomal stability of 76%–100%[1].

ln Vivo

Following oral administration, the absolute bioavailability was moderate in rats (45%) and high in mice (∼100%). GLPG0634 (30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)) dose-dependently reduces inflammation, cartilage, and bone degradation in the CIA model in rats and mice.

Animal Protocol

Dissolved in 0.5% (v/v) methylcellulose; 30 mg/kg (Rats) and 50 mg/kg (Mice); Oral administration

Rat and mouse CIA model

References

[1]. Christel Jeanne Marie Menet, et al. Novel compounds useful for the treatment of degenerative and inflammatory diseases. WO2010010190A1.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C23H18N6O2

Molecular Weight

410.43

CAS #

1206101-20-3

Related CAS #

Filgotinib;1206161-97-8

SMILES

O=C(C1CC1)NC2=NN3C(C4=CC=C(OCC5=CC=C(C#N)N=C5)C=C4)=CC=CC3=N2

Synonyms

Filgotinib-analogue; GLPG-0634 analogue;Filgotinib analogue, GLPG0634 analog; GLPG 0634 analogue; GLPG 0634 analogue

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 0.1 mg/mL (0.24 mM)

Water:<1 mg/mL

Ethanol:<1 mg/mL

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4365 mL	12.1823 mL	24.3647 mL
	5 mM	0.4873 mL	2.4365 mL	4.8729 mL
	10 mM	0.2436 mL	1.2182 mL	2.4365 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

Calculate Reset

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculate Reset

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in 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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate Reset

Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05323591	Recruiting	Drug: Filgotinib	Rheumatoid Arthritis	Galapagos NV	May 3, 2022
NCT03926195	Completed Has Results	Drug: Filgotinib Drug: Placebo	Rheumatoid Arthritis Psoriatic Arthritis	Galapagos NV	May 28, 2019	Phase 2
NCT06285539	Not yet recruiting	Drug: Filgotinib	Behcet's Disease Idiopathic Inflammatory Myopathies	UMC Utrecht	March 2024	Phase 2
NCT05697159	Recruiting	Drug: Larotrectinib Sulfate Procedure: Bone Scan	Rheumatoid Arthritis Sickness Behavior	NHS Greater Glasgow and Clyde	August 22, 2023

Biological Data

GLPG0634 inhibits the differentiation of Th1, Th2, and Th17 cells.J Immunol.2013 Oct 1;191(7):3568-77.
GLPG0634 dose-dependently prevents disease progression in the therapeutic rat CIA model.J Immunol.2013 Oct 1;191(7):3568-77.
GLPG0634 is efficacious in a mouse therapeutic CIA model.J Immunol.2013 Oct 1;191(7):3568-77.