Ziritaxestat (Synonyms: GLPG1690)

Name: Ziritaxestat
Brand: MedChemExpress
SKU: HY-101772
Rating: 5.0 (5 reviews)

Cat. No.: HY-101772 Purity: 99.93%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

Ziritaxestat Chemical Structure

CAS No. : 1628260-79-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 71	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 71	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Ziritaxestat

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•Related Screening Libraries:

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View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Purity & Documentation
References
Customer Review

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)

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.

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.

Clinical Trial

Molecular Weight

588.70

Formula

C₃₀H₃₃FN₈O₂S

CAS No.

1628260-79-6

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 41.67 mg/mL (70.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.

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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.93%

Select Batch:

Data Sheet (273 KB) SDS (641 KB)

COA (248 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Ziritaxestat Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ziritaxestat1628260-79-6GLPG1690GLPG 1690GLPG-1690Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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Ziritaxestat (Synonyms: GLPG1690)

Customer Review

Ziritaxestat Related Antibodies

5 Publications Citing Use of MCE Ziritaxestat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Ziritaxestat Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Ziritaxestat Related Classifications

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