Ziritaxestat
CAS No. : 1628260-79-6
(Synonyms: GLPG1690)
| Size | Price | Stock |
|---|---|---|
| 5mg | $55 | In-stock |
| 10mg | $90 | In-stock |
| 25mg | $150 | In-stock |
| 50mg | $250 | In-stock |
| 100mg | $450 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-101772 |
| M.Wt: | 588.70 |
| Formula: | C30H33FN8O2S |
| Purity: | >98 % |
| Solubility: | DMSO : 41.67 mg/mL (ultrasonic) |
Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM[1].
IC50 & Target: IC50: 131 nM (ATX)[1]
Ki: 15 nM (ATX)[1]
In Vitro: Ziritaxestat (GLPG1690) shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay[1].
In Vivo: Ziritaxestat (GLPG1690) 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.Ziritaxestat (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 Ziritaxestat (GLPG1690) showing low plasma clearance (0.12 L/h/kg) and a high bioavailability (63%)[1].
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