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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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Z414252-5mg | 5mg | In stock | $53.90 | |
Z414252-10mg | 10mg | In stock | $88.90 | |
Z414252-25mg | 25mg | In stock | $147.90 | |
Z414252-50mg | 50mg | In stock | $246.90 | |
Z414252-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $444.90 |
PDE Inhibitors
Synonyms | (2-Amino-4-oxo-4,5-dihydro-1,3-thiazol-5-yl)acetic acid # | AC-36149 | GLPG-1690(Ziritaxestat) | MFCD31544330 | Ziritaxestat [USAN] | WHO 11017 | GTPL9561 | 2-[[2-Ethyl-8-Methyl-6-[4-[2-(3-Oxidanylazetidin-1-Yl)-2-Oxidanylidene-Ethyl]piperazin-1-Yl]imidaz |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Autotaxin inhibitor |
Product Description | Information Ziritaxestat (GLPG1690) Ziritaxestat (GLPG1690) is a selective autotaxin inhibitor with an IC50 of 131 nM and Ki of 15 nM. Targets Autotaxin 15 nM(Ki) In vivo Ziritaxestat (GLPG1690) decreases LPA levels in a sustainable manner, in mouse plasma, from a dose of 3 mg/kg onward. It demonstrates significant activity in the mouse BLM-induced fibrosis model at doses of 10 and 30 mg/kg twice a day. |
ALogP | 4.8 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 2-[[2-ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]-methylamino]-4-(4-fluorophenyl)-1,3-thiazole-5-carbonitrile |
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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 |
InChi Key | REQQVBGILUTQNN-UHFFFAOYSA-N |
Canonical SMILES | CCC1=C(N2C=C(C=C(C2=N1)C)N3CCN(CC3)CC(=O)N4CC(C4)O)N(C)C5=NC(=C(S5)C#N)C6=CC=C(C=C6)F |
Isomeric SMILES | CCC1=C(N2C=C(C=C(C2=N1)C)N3CCN(CC3)CC(=O)N4CC(C4)O)N(C)C5=NC(=C(S5)C#N)C6=CC=C(C=C6)F |
PubChem CID | 90420193 |
Molecular Weight | 588.7 |
PubChem CID | 90420193 |
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ChEMBL Ligand | CHEMBL3828074 |
CAS Registry No. | 1628260-79-6 |
RCSB PDB Ligand | 7NB |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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F2208282 | Certificate of Analysis | May 20, 2022 | Z414252 |
F2208283 | Certificate of Analysis | May 20, 2022 | Z414252 |
F2208287 | Certificate of Analysis | May 20, 2022 | Z414252 |
F2208288 | Certificate of Analysis | May 20, 2022 | Z414252 |
F2208289 | Certificate of Analysis | May 20, 2022 | Z414252 |
Solubility | Solubility (25°C) In vitro DMSO: 100 mg/mL (169.86 mM); Ethanol: 4 mg/mL (6.79 mM); Water: Insoluble; |
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Pictogram(s) | GHS08, GHS07 |
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Signal | Danger |
Hazard Statements | H373:Causes damage to organs through prolonged or repeated exposure H302:Harmful if swallowed H360:May damage fertility or the unborn child |
Precautionary Statements | P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Zhao Y, Natarajan V. (2013) Lysophosphatidic acid (LPA) and its receptors: role in airway inflammation and remodeling.. Biochim Biophys Acta, 1831 (1): (86-92). [PMID:22809994] [10.1021/op500134e] |
2. Park GY, Lee YG, Berdyshev E, Nyenhuis S, Du J, Fu P, Gorshkova IA, Li Y, Chung S, Karpurapu M et al.. (2013) Autotaxin production of lysophosphatidic acid mediates allergic asthmatic inflammation.. Am J Respir Crit Care Med, 188 (8): (928-40). [PMID:24050723] [10.1021/op500134e] |
3. Bain G, Shannon KE, Huang F, Darlington J, Goulet L, Prodanovich P, Ma GL, Santini AM, Stein AJ, Lonergan D et al.. (2017) Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.. J Pharmacol Exp Ther, 360 (1): (1-13). [PMID:27754931] [10.1021/op500134e] |
4. Desroy N, Housseman C, Bock X, Joncour A, Bienvenu N, Cherel L, Labeguere V, Rondet E, Peixoto C, Grassot JM et al.. (2017) Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fibrosis.. J Med Chem, 60 (9): (3580-3590). [PMID:28414242] [10.1021/op500134e] |
5. Orosa B, García S, Conde C. (2015) The autotaxin-lysophosphatidic acid pathway in pathogenesis of rheumatoid arthritis.. Eur J Pharmacol, 765 (13): (228-33). [PMID:26297977] [10.1021/op500134e] |
6. Maher TM, Kreuter M, Lederer DJ, Brown KK, Wuyts W, Verbruggen N, Stutvoet S, Fieuw A, Ford P, Abi-Saab W et al.. (2019) Rationale, design and objectives of two phase III, randomised, placebo-controlled studies of GLPG1690, a novel autotaxin inhibitor, in idiopathic pulmonary fibrosis (ISABELA 1 and 2).. BMJ Open Respir Res, 6 (1): (e000422). [PMID:31179008] [10.1021/op500134e] |
7. Tang X, Wuest M, Benesch MGK, Dufour J, Zhao Y, Curtis JM, Monjardet A, Heckmann B, Murray D, Wuest F et al.. (2020) Inhibition of Autotaxin with GLPG1690 Increases the Efficacy of Radiotherapy and Chemotherapy in a Mouse Model of Breast Cancer.. Mol Cancer Ther, 19 (1): (63-74). [PMID:31548293] [10.1021/op500134e] |
8. Benesch MGK, Tang X, Brindley DN. (2020) Autotaxin and Breast Cancer: Towards Overcoming Treatment Barriers and Sequelae.. Cancers (Basel), 12 (2): (1755-70). [PMID:32041123] [10.1021/op500134e] |
9. Feng Y, Mischler WJ, Gurung AC, Kavanagh TR, Androsov G, Sadow PM, Herbert ZT, Priolo C. (2020) Therapeutic Targeting of the Secreted Lysophospholipase D Autotaxin Suppresses Tuberous Sclerosis Complex-Associated Tumorigenesis.. Cancer Res, 80 (13): (2751-2763). [PMID:32393662] [10.1021/op500134e] |