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GS-829845

SKU: orb1741358

Description

GS-829845 is the primary active metabolite of the JAK1 inhibitor Filgotinib. It exhibits a longer half-life and approximately 10-fold lower potency than its parent compound. This small molecule is used in research to investigate JAK-STAT signaling in inflammatory and autoimmune disease models, both in vitro and in vivo.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number1257705-09-1
MW357.43
Purity99.93%
FormulaC17H19N5O2S
SMILESNc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1
TargetDrug Metabolite,JAK
SolubilityDMSO:90 mg/mL (251.8 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (9.23 mM)

Bioactivity

In Vivo
Filgotinib did not alter metformin exposures, indicating that filgotinib and GS-829845 do not inhibit OCT2 and MATE1/2K at the clinical doses. Filgotinib was generally well-tolerated when administered alone or with the co-administered drugs in the studies. Results from these studies were the basis to enable the use of P-gp modulators and substrates of OCT2, MATE1, and MATE2K with filgotinib without the need for dose modifications in the current approved rheumatoid arthritis population.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Drug Metabolite, DrugMetabolite, JAK1, GS 829845, GS829845, GS-829845
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

GS-829845 (orb1741358)

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% Tween 80 +
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Available Sizes

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5 mg
¥ 1,040.00
10 mg
¥ 1,300.00
25 mg
¥ 1,690.00
50 mg
¥ 2,210.00
DispatchUsually dispatched within 3-5 working days
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