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GLPG1690

Cat. No. M6287
GLPG1690 Structure
Synonym:

Ziritaxestat

Size Price Availability Quantity
5mg USD 48  USD48 In stock
10mg USD 80  USD80 In stock
25mg USD 136  USD136 In stock
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Quality Control & Documentation
Biological Activity

In vitro: GLPG1690 (Ziritaxestat) shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay.

In vivo: GLPG1690 (Ziritaxestat) inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma in a concentration-dependent manner, with IC50 values of 418 nM, 542 nM, and 242 nM, respectively. GLPG1690 displays improved pharmacokinetic properties, with a low plasma clearance and high bioavailability in mouse and rat. The good pharmacokinetic profile is further confirmed in dog, with GLPG1690 showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%).

Chemical Information
Molecular Weight 588.7
Formula C30H33FN8O2S
CAS Number 1628260-79-6
Solubility (25°C) 10 mM in DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Balupuri A, et al. Bioorg Med Chem Lett. Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.

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Keywords: GLPG1690, Ziritaxestat supplier, PDE, inhibitors, activators


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