GLPG1690
Modify Date: 2024-01-11 12:18:50
GLPG1690 structure
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Common Name | GLPG1690 | ||
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| CAS Number | 1628260-79-6 | Molecular Weight | 588.699 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C30H33FN8O2S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of GLPG1690GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM. |
| Name | 2-[[2-Ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)-5-thiazolecarbonitrile |
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| Synonym | More Synonyms |
| Description | GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM. |
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| Related Catalog | |
| Target |
IC50: 131 nM (ATX)[1] Ki: 15 nM (ATX)[1] |
| In Vitro | GLPG1690 shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC50 of 15 μM in manual patch clamp assay[1]. |
| In Vivo | 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. 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%)[1]. |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C30H33FN8O2S |
| Molecular Weight | 588.699 |
| Exact Mass | 588.243103 |
| LogP | 2.48 |
| Index of Refraction | 1.714 |
| schembl16051264 |
| 2-[(2-Ethyl-6-{4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl}-8-methylimidazo[1,2-a]pyridin-3-yl)(methyl)amino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile |
| unii-i02418v13w |
| 5-Thiazolecarbonitrile, 2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)- |
| GLPG1690 |
| GLPG-1690 |