Cat. No.: HY-101772

Ziritaxestat

Name: Ziritaxestat
Brand: MedChemExpress
SKU: HY-101772
Price: 55.00 USD
Availability: InStock
Rating: 5 (7 reviews)

(Synonyms: GLPG1690)

7 Cited Publications

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Based on 7 publication(s) in Google Scholar

Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC₅₀ of 131 nM and a K_i of 15 nM.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté : 99.93%
CAS No.: 1628260-79-6
Formule: C₃₀H₃₃FN₈O₂S
Masse moléculaire:588.70

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ziritaxestat Chemical Structure

CAS No.: 1628260-79-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (7)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole (1)
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Ziritaxestat (GLPG1690) is a first-in-class autotaxin (ATX) inhibitor, with an IC₅₀ of 131 nM and a K_i of 15 nM^[1].

IC₅₀ & Target

^[1]

Autotaxin

131 nM (IC₅₀)

Autotaxin

15 nM (Ki)

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>15 μM Compound: GLPG-1690	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 32535330]
A549	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
Hep 3B2	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human Hep3B cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
MCF7	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
MCF7	IC₅₀	8.32 μM Compound: GLPG-1690	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 32535330]
MDA-MB-231	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
MDA-MB-231	IC₅₀	6.27 μM Compound: GLPG-1690	Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay	[PMID: 32535330]
NCI-H1581	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human NCI-H1581 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
NCI-H2228	IC₅₀	>15 μM Compound: GLPG-1690	Antiproliferative activity against human NCI-H2228 cells measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H2228 cells measured after 72 hrs by MTT assay	[PMID: 32535330]
NCI-H2228	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against human H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]
RAW264.7	IC₅₀	>20 μM Compound: 4; GLPG1690	Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35436669]

In Vitro

Ziritaxestat (GLPG1690) shows no CYP3A4 TDI and decreases hERG inhibitory activity with IC₅₀ of 15 μM in manual patch clamp assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1628260-79-6
Appearance Solid
Masse moléculaire 588.70
Formule C₃₀H₃₃FN₈O₂S
Color White to off-white
SMILES

N#CC1=C(C2=CC=C(F)C=C2)N=C(N(C3=C(CC)N=C4C(C)=CC(N5CCN(CC(N6CC(O)C6)=O)CC5)=CN43)C)S1
Synonyms

GLPG1690
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (7)

All Flow CytometryCell Proliferation/Viability AssayCell Migration/Invasion AssayIn Vivo Efficacy Study

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Journal Impact Factor

Immunity

Plasmacytoid dendritic cell activation is dependent on coordinated expression of distinct amino acid transporters. [Abstract]

2021 Nov 9;54(11):2514-2530.e7. PMID: 34717796

Ziritaxestat purchased from MedChemExpress. Usage Cited in: Immunity. 2021 Nov 9;54(11):2514-2530.e7. [Abstract]

Isolated pDCs were maintained in HPLM ± IL-3 with Ziritaxestat (ZIR; 10-30 μM) o/n then stimulated ± CpG-A for 5 h and probed for: kynurenine uptake, pS6 expression and IFN-α production.
Pharmacol Res

ENPP2 inhibitor improves proliferation in AOM/DSS-induced colorectal cancer mice via remodeling the gut barrier function and gut microbiota composition. [Abstract]

2023 Sep:195:106877. PMID: 37524154

Ziritaxestat purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2023 Sep:195:106877. [Abstract]

GLPG1690 (Ziritaxestat; 7.5-20 μM; 48 h) treatment significantly increased the percentage of apoptotic cells in HT29 and HCT116 cells.
EBioMedicine

A SNP of bacterial blc disturbs gut lysophospholipid homeostasis and induces inflammation through epithelial barrier disruption. [Abstract]

2020 Feb:52:102652. PMID: 32058942
Cancer Immunol Res

Ex Vivo Immuno-Oncology Platform Reveals Spatial T Cell Infiltration Patterns Linked to ATR Inhibition Responses in High-Grade Serous Ovarian Cancer. [Abstract]

2026 Jan 21:10.1158/2326-6066.CIR-25-0743. PMID: 41563843
RSC Adv

A multi-stage computational pipeline and in vitro validation for the discovery of small-molecule translation inhibitors targeting the bacterial ribosome. [Abstract]

2026 Apr 7;16(20):18359-18373. PMID: 41953617
Cancer Sci

Dual role of autotaxin as novel biomarker and therapeutic target in pancreatic neuroendocrine neoplasms. [Abstract]

2023 Dec;114(12):4571-4582. PMID: 37770812

Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]

Cell proliferation by ATX inhibitor (GLPG1690, Ziritaxestat; 48 h) in QGP-1 and BON-1. Data represent means of the control group with dimethyl sulfoxide (DMSO) (n = 4) and treatment group with GLPG1690 (n = 4). Daily treatment was GLPG1690 at 10 μmol/L in QGP-1 and BON-1 or equivalent amount of DMSO.

Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]

Ziritaxestat (GLPG1690; 10 μM; 24 h) suppressed the migration of BON-1 cells.

Ziritaxestat purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2023 Dec;114(12):4571-4582. [Abstract]

Ziritaxestat (GLPG1690; 60 mg/kg; i.p.; once daily for 13 days) attenuated tumor growth in a BON-1 xenograft mouse model.
bioRxiv

2024 Feb 19.

Solvant et solubilité

In Vitro:

DMSO : 40 mg/mL (67.95 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6987 mL

8.4933 mL

16.9866 mL

5 mM

0.3397 mL

1.6987 mL

3.3973 mL

10 mM

0.1699 mL

0.8493 mL

1.6987 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 15% Cremophor EL 85% Saline

Solubility: 20 mg/mL (33.97 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
SDS (643 KB)
- English - EN (643 KB)
- Français - FR (643 KB)
- Deutsch - DE (643 KB)
- Norwegian - NO (643 KB)
- Español - ES (643 KB)
- Swedish - SV (643 KB)
- Italian - IT (643 KB)
- Korean - KR (643 KB)
- Portuguese - PT (643 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Desroy N, et al. 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. 2017 May 11;60(9):3580-3590. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6987 mL	8.4933 mL	16.9866 mL	42.4665 mL
	5 mM	0.3397 mL	1.6987 mL	3.3973 mL	8.4933 mL
	10 mM	0.1699 mL	0.8493 mL	1.6987 mL	4.2466 mL
	15 mM	0.1132 mL	0.5662 mL	1.1324 mL	2.8311 mL
	20 mM	0.0849 mL	0.4247 mL	0.8493 mL	2.1233 mL
	25 mM	0.0679 mL	0.3397 mL	0.6795 mL	1.6987 mL
	30 mM	0.0566 mL	0.2831 mL	0.5662 mL	1.4155 mL
	40 mM	0.0425 mL	0.2123 mL	0.4247 mL	1.0617 mL
	50 mM	0.0340 mL	0.1699 mL	0.3397 mL	0.8493 mL
	60 mM	0.0283 mL	0.1416 mL	0.2831 mL	0.7078 mL

Bioz

Keywords

Ziritaxestat

7 Cited Publications

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Ziritaxestat

Publications Citing Use of MedChemExpress (MCE) Ziritaxestat

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)