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

Ziritaxestat  (Synonyms: GLPG1690)

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

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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Solution
10 mM * 1 mL in DMSO USD 71 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 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
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Customer Review

Based on 2 publication(s) in Google Scholar

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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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

588.70

Appearance

Solid

Formula

C30H33FN8O2S
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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:  5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (4.25 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

  • 3.

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

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.29%

COA (247 KB) HNMR (293 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References
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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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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

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

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