1. Neuronal Signaling
  2. Monoamine Oxidase
  3. LOX-IN-3

LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and angiogenesis research.

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

LOX-IN-3 Chemical Structure

LOX-IN-3 Chemical Structure

CAS No. : 2409963-83-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 418 In-stock
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
5 mg USD 380 In-stock
10 mg USD 600 In-stock
25 mg USD 1150 In-stock
50 mg USD 1800 In-stock
100 mg USD 2850 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and angiogenesis research[1].

IC50 & Target

IC50: <1 μM (human LOXL2), <10 μM (bovine LOX)[1]

In Vitro

LOX-IN-3 dihydrochloride monohydrate (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50 values of <10 μM and <1 μM, respectively[1].
LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2[1].
LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities[1].

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

In Vivo

LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1].
LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1].
LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1].

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

Animal Model: Male Wistar rats[1]
Dosage: 30 mg/kg
Administration: Oral administration, single dose
Result: Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta).
Animal Model: Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage, daily for 14 days
Result: Increased kidney weight and thickness and reduced the area of fibrosis.
Animal Model: C57Bl/6 mice, Bleomycin-induced lung fibrosis model
Dosage: 15 mg/kg
Administration: Oral gavage, daily for 21 days
Result: Significantly reduced the Ashcroft score and the lung weight.
Molecular Weight

280.32

Formula

C13H13FN2O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC/C=C(F)/CS(=O)(C1=C2N=CC=CC2=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (445.92 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 3.5674 mL 17.8368 mL 35.6735 mL
5 mM 0.7135 mL 3.5674 mL 7.1347 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 (protect from light). 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 (7.42 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.42 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.97%

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 (protect from light). 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 3.5674 mL 17.8368 mL 35.6735 mL 89.1838 mL
5 mM 0.7135 mL 3.5674 mL 7.1347 mL 17.8368 mL
10 mM 0.3567 mL 1.7837 mL 3.5674 mL 8.9184 mL
15 mM 0.2378 mL 1.1891 mL 2.3782 mL 5.9456 mL
20 mM 0.1784 mL 0.8918 mL 1.7837 mL 4.4592 mL
25 mM 0.1427 mL 0.7135 mL 1.4269 mL 3.5674 mL
30 mM 0.1189 mL 0.5946 mL 1.1891 mL 2.9728 mL
40 mM 0.0892 mL 0.4459 mL 0.8918 mL 2.2296 mL
50 mM 0.0713 mL 0.3567 mL 0.7135 mL 1.7837 mL
60 mM 0.0595 mL 0.2973 mL 0.5946 mL 1.4864 mL
80 mM 0.0446 mL 0.2230 mL 0.4459 mL 1.1148 mL
100 mM 0.0357 mL 0.1784 mL 0.3567 mL 0.8918 mL
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LOX-IN-3 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.

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LOX-IN-3
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