GLPG0634 analogue

Catalog No.S7137 Batch:S713701

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Technical Data

Formula

C23H18N6O2

Molecular Weight 410.43 CAS No. 1206101-20-3
Solubility (25°C)* In vitro DMSO 0.1 mg/mL (0.24 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
Targets
JAK [1]
In vitro In cell lines, GLPG0634 inhibits IL-2- and IL-4-induced JAK1/JAK3/γc signaling and IFN-αB2-induced JAK1/TYK2 type II receptor signaling with IC50 ranged from 150 to 760 nM. GLPG0634 shows higher selectivity for JAK/STAT signaling involving JAK1 than JAK2 kinase in a cellular context. Besides, GLPG0634 also inhibits the differentiation of Th1, Th2, and Th17 cells. [1]
In 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. [1]

Protocol (from reference)

Animal Study:

[1]

  • Animal Models

    Rat CIA model and mouse CIA model

  • Dosages

    30 mg/kg daily (Rats); 50 mg/kg twice daily (Mice)

  • Administration

    p.o.

Customer Product Validation

Data from [Data independently produced by , , Erasmus University Rotterdam, thesis, 2016]

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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