2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. ATX inhibitor 5

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.

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

ATX inhibitor 5 Chemical Structure

ATX inhibitor 5 Chemical Structure

CAS No. : 2402772-45-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 303 In-stock
Solution
10 mM * 1 mL in DMSO USD 303 In-stock
Solid
5 mg USD 290 In-stock
10 mg USD 465 In-stock
25 mg USD 790 In-stock
50 mg USD 1080 In-stock
100 mg USD 1480 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

ATX inhibitor 5 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently[1].

IC50 & Target[1]

Autotaxin

 

In Vitro

ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC)[1].
ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β[1].

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

ATX inhibitor 5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: CFs and t-HSC/Cl-6 cells
Concentration: 0.0001, 0.01, 1, 100, 10000 µM
Incubation Time: 48 hours
Result: Displayed activities against CFs and t-HSC/Cl-6 cells with IC50s of 1.21 and 0.78 µM, respectively.
In Vivo

ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently[1].

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

Animal Model: Male Konmin mice (8-week old, 22-25 g)[1]
Dosage: 20, 40 mg/kg
Administration: Orally; once daily for two weeks
Result: Prominently reduced CCl4-induced hepatic fibrosis level.
Molecular Weight

474.87

Formula

C22H18ClF3N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N/N=C/C1=CC=C(Cl)C=C1)N(C2)CCC3=C2C(NC4=CC=CC(C(F)(F)F)=C4)=NC=N3
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 : 250 mg/mL (526.46 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 2.1058 mL 10.5292 mL 21.0584 mL
5 mM 0.4212 mL 2.1058 mL 4.2117 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.38 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 2

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

    Solubility: ≥ 2.08 mg/mL (4.38 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.

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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1058 mL 10.5292 mL 21.0584 mL 52.6460 mL
5 mM 0.4212 mL 2.1058 mL 4.2117 mL 10.5292 mL
10 mM 0.2106 mL 1.0529 mL 2.1058 mL 5.2646 mL
15 mM 0.1404 mL 0.7019 mL 1.4039 mL 3.5097 mL
20 mM 0.1053 mL 0.5265 mL 1.0529 mL 2.6323 mL
25 mM 0.0842 mL 0.4212 mL 0.8423 mL 2.1058 mL
30 mM 0.0702 mL 0.3510 mL 0.7019 mL 1.7549 mL
40 mM 0.0526 mL 0.2632 mL 0.5265 mL 1.3161 mL
50 mM 0.0421 mL 0.2106 mL 0.4212 mL 1.0529 mL
60 mM 0.0351 mL 0.1755 mL 0.3510 mL 0.8774 mL
80 mM 0.0263 mL 0.1316 mL 0.2632 mL 0.6581 mL
100 mM 0.0211 mL 0.1053 mL 0.2106 mL 0.5265 mL
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ATX inhibitor 5 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:

ATX inhibitor 52402772-45-4ATX inhibitor5ATX inhibitor-5Phosphodiesterase (PDE)fibrosisdiseasescardiacfibroblastsCFshepaticstellatecellHSCanti-hepatofibrosisanti-proliferative,Inhibitorinhibitorinhibit

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