2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. Ziritaxestat

Ziritaxestat  (Synonyms: GLPG1690)

Cat. No.: HY-101772 Purity: 99.29%
COA Handling Instructions

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Ziritaxestat (GLPG1690) est un inhibiteur de autotaxine (ATX) de première classe, avec un IC50 de 131 nM et un Ki sur 15 nM.

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

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

Ziritaxestat Chemical Structure

Ziritaxestat Chemical Structure

CAS No. : 1628260-79-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 71 In-stock
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10 mM * 1 mL in DMSO USD 71 In-stock
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10 mg USD 90 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Ziritaxestat Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

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 Ki of 15 nM[1].

IC50 & Target[1]

Autotaxin

131 nM (IC50)

Autotaxin

15 nM (Ki)

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.

Ziritaxestat Related Antibodies
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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.29%

COA (248 KB) HNMR (293 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References

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.

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
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Ziritaxestat Related Classifications

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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