Description
Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and a Ki of 15 nM.
Product information
CAS Number: 1628260-79-6
Molecular Weight: 588.70
Formula: C30H33FN8O2S
Chemical Name: 2-[(2-ethyl-6-{4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl}-8-methylimidazo[1,2-a]pyridin-3-yl)(methyl)amino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile
Smiles: CN(C1=NC(=C(C#N)S1)C1C=CC(F)=CC=1)C1=C(CC)N=C2C(C)=CC(=CN21)N1CCN(CC(=O)N2CC(O)C2)CC1
InChiKey: REQQVBGILUTQNN-UHFFFAOYSA-N
InChi: InChI=1S/C30H33FN8O2S/c1-4-24-29(35(3)30-34-27(25(14-32)42-30)20-5-7-21(31)8-6-20)39-15-22(13-19(2)28(39)33-24)37-11-9-36(10-12-37)18-26(41)38-16-23(40)17-38/h5-8,13,15,23,40H,4,9-12,16-18H2,1-3H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 41.67 mg/mL (70.78 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Ziritaxestat (GLPG1690) shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay.
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%).
Products are for research use only. Not for human use.
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