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GS-829845

Catalog No. T67905   CAS 1257705-09-1

GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.

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GS-829845 Chemical Structure
GS-829845, CAS 1257705-09-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 57.00
25 mg In stock $ 90.00
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Purity: 99.78%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GS-829845 is a JAK1 inhibitor, the main component of the active metabolite of Filgotinib, which is approximately 10-fold less potent and has a longer half-life than the parent.
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.[2]
Molecular Weight 357.43
Formula C17H19N5O2S
CAS No. 1257705-09-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90.0 mg/mL (251.8 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Meng A, et al. Exposure-response relationships for the efficacy and safety of filgotinib and its metabolite GS-829845 in subjects with rheumatoid arthritis based on phase 2 and phase 3 studies. Br J Clin Pharmacol. 2022;88(7):3211-3221. 2. Hsueh CH, et al. Evaluation of the potential drug interactions mediated through P-gp, OCT2, and MATE1/2K with filgotinib in healthy subjects. Clin Transl Sci. 2022;15(2):361-370. 3. Namour F, et al. Filgotinib: A Clinical Pharmacology Review. Clin Pharmacokinet. 2022;61(6):819-832.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets
Dehydrocrenatidine STAT3-IN-18 Abrocitinib JAK-IN-34 RO495 Pyridone 6 Ritlecitinib QL-1200186

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Keywords

GS-829845 1257705-09-1 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Metabolism Stem Cells JAK Drug Metabolite GS 829845 GS829845 inhibitor inhibit

 

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