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

Ziritaxestat (Synonyms: GLPG1690)

Cat. No.: HY-101772 Purity: 99.97%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
25 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
100 mg USD 588 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

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].

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (70.78 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 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

*All of the co-solvents are provided by MCE.
References
Molecular Weight

588.70

Formula

C₃₀H₃₃FN₈O₂S

CAS No.

1628260-79-6

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

Purity: 99.97%

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Product Name:
Ziritaxestat
Cat. No.:
HY-101772
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Ziritaxestat

Cat. No.: HY-101772