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Chemical Structure| 1628260-79-6 Chemical Structure| 1628260-79-6

Structure of Ziritaxestat
CAS No.: 1628260-79-6

Chemical Structure| 1628260-79-6

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GLPG1690, a first-in-class autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nMl, is able to cause a sustained reduction of LPA levels in plasma in vivo and was shown to be efficacious in a bleomycin-induced pulmonary fibrosis model in mice, and in reducing extra-cellular matrix deposition in the lung whilst also reducing LPA 18:2 content in bronchoalveolar lavage fluid and may be a possible effectvie compound in treating idiopathic pulmonary fibrosis.

Synonyms: GLPG1690

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Product Details of Ziritaxestat

CAS No. :1628260-79-6
Formula : C30H33FN8O2S
M.W : 588.70
SMILES Code : N#CC1=C(C2=CC=C(F)C=C2)N=C(N(C3=C(CC)N=C4C(C)=CC(N5CCN(CC(N6CC(O)C6)=O)CC5)=CN43)C)S1
Synonyms :
GLPG1690
MDL No. :MFCD31544330
InChI Key :REQQVBGILUTQNN-UHFFFAOYSA-N
Pubchem ID :90420193

Safety of Ziritaxestat

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BON-1 10 µM 24 hours Inhibition of cell proliferation and migration Cancer Sci. 2023 Dec;114(12):4571-4582
QGP-1 10 µM 24 hours Inhibition of cell proliferation and migration Cancer Sci. 2023 Dec;114(12):4571-4582
LAM patient renal angiomyolipoma-derived TSC2-deficient cells (621-102) 6 µM 24 hours To assess the effect of GLPG1690 on the proliferation of TSC2-deficient cells, results showed that GLPG1690 inhibited the proliferation of TSC2-deficient cells. Cancer Res. 2020 Jul 1;80(13):2751-2763
Tsc2−/− mouse embryonic fibroblasts (MEFs) 3 µM 68 hours To assess the effect of GLPG1690 on the proliferation of Tsc2−/− MEFs, results showed that GLPG1690 inhibited the proliferation of Tsc2−/− MEFs. Cancer Res. 2020 Jul 1;80(13):2751-2763

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice (BALB/c Slc-nu/nu) Xenograft model Intraperitoneal injection 60 mg/kg Once daily for 13 days Suppression of tumor growth Cancer Sci. 2023 Dec;114(12):4571-4582
NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice Subcutaneous tumor model Intraperitoneal injection 60 mg/kg/day Once daily for 30 days To assess the inhibitory effect of GLPG1690 on TSC tumor growth, results showed that GLPG1690 reduced tumor volume by approximately 40%. Cancer Res. 2020 Jul 1;80(13):2751-2763
Human Patients with idiopathic pulmonary fibrosis Oral 600 mg or 200 mg Once daily for at least 52 weeks To evaluate the efficacy and safety of GLPG1690 in patients with idiopathic pulmonary fibrosis, with the primary endpoint being the rate of decline in FVC over 52 weeks. BMJ Open Respir Res. 2019 May 21;6(1):e000422

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03976648 Systemic Sclerosis PHASE2 TERMINATED 2021-04-13 Pacific Arthritis Care Center,... More >> Los Angeles, California, 90045, United States|UCLA Rheumatology, Los Angeles, California, 90095, United States|RASF Clinical Research Center, Boca Raton, Florida, 33486, United States|University of Michigan, Ann Arbor, Michigan, 48109, United States|Metroplex Clinical Research Center, Dallas, Texas, 75231, United States|UT Physicians Center for Autoimmunity, Houston, Texas, 77030, United States|UZ Gent, Gent, 9000, Belgium|UZ Leuven, Leuven, 3000, Belgium|Azienda Ospedaliero Universitaria Careggi, Firenze, 50139, Italy|Ospedale San Raffaele S.r.l. - PPDS, Milano, 20132, Italy|Hospital Universitario Vall d'Hebron, Barcelona, 8035, Spain|Hospital Universitario 12 de Octubre, Madrid, 28041, Spain|University Hospital Aintree, Liverpool, L9 7AL, United Kingdom|Royal Free Hospital, London, NW32QG, United Kingdom Less <<
NCT03143712 Healthy PHASE1 COMPLETED 2017-06-14 SGS CPU, Antwerp, Belgium

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.49mL

1.70mL

0.85mL

16.99mL

3.40mL

1.70mL

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