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GLPG1690

Cat. No. M6287
GLPG1690 Structure
Synonym:

Ziritaxestat

Size Price Availability Quantity
5mg USD 84 In stock
10mg USD 110 In stock
25mg USD 227 In stock
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Quality Control
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%).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 588.7
Formula C30H33FN8O2S
CAS Number 1628260-79-6
Purity 98.35%
Solubility 10 mM in DMSO
Storage at -20°C
References

Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.
Balupuri A, et al. Bioorg Med Chem Lett. 2017 Sep 1;27(17):4156-4164. PMID: 28743508.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GLPG1690, Ziritaxestat supplier, PDE, inhibitors

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