2. Neuronal Signaling
  3. Monoamine Oxidase
  4. Lenumlostat

Lenumlostat  (Synonyms: PAT-1251; GB2064)

Cat. No.: HY-107422 Purity: 99.92%
COA Handling Instructions

Molarity Calculator

PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases.

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

Lenumlostat Chemical Structure

Lenumlostat Chemical Structure

CAS No. : 2007885-39-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 660 In-stock
Solution
10 mM * 1 mL in DMSO USD 660 In-stock
Solid
5 mg USD 600 In-stock
10 mg USD 840 In-stock
25 mg USD 1400 In-stock
50 mg USD 1830 In-stock
100 mg USD 2380 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lenumlostat:

Lenumlostat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lenumlostat

View All Monoamine Oxidase Isoform Specific Products:

View All Isoforms
MAO-A MAO-B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases[1].

IC50 & Target

IC50: 0.10 μM (Mouse LOXL2), 0.12 μM (Rat LOXL2), 0.16 μM (Dog LOXL2), 0.71 μM (hLOXL2), 1.17 μM (hLOXL3)[1]
In Vitro

PAT-1251 is a Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 shows highly selective for LOXL2 over other key members of the amine oxidase family, such as the copper-dependent amine oxidases semicarbazide-sensitive amine oxidase (SSAO) and diamine oxidase (DAO), in addition to the flavin-dependent monoamine oxidases A (MAO-A) and B (MAO-B), with <10% inhibition at 10 μM[1].

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

Lenumlostat Related Antibodies
Clinical Trial
Molecular Weight

399.34

Formula

C18H17F4N3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC=CC(OC2=NC(C(F)(F)F)=CC(CN)=C2)=C1)N3C[C@@H](F)[C@H](O)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 130 mg/mL (325.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 100 mg/mL (250.41 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5041 mL 12.5207 mL 25.0413 mL
5 mM 0.5008 mL 2.5041 mL 5.0083 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.17 mg/mL (5.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (5.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.92%

COA (245 KB) HNMR (315 KB) LCMS (270 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, 6 months; -20°C, 1 month (stored under nitrogen). 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
H2O / DMSO 1 mM 2.5041 mL 12.5207 mL 25.0413 mL 62.6033 mL
5 mM 0.5008 mL 2.5041 mL 5.0083 mL 12.5207 mL
10 mM 0.2504 mL 1.2521 mL 2.5041 mL 6.2603 mL
15 mM 0.1669 mL 0.8347 mL 1.6694 mL 4.1736 mL
20 mM 0.1252 mL 0.6260 mL 1.2521 mL 3.1302 mL
25 mM 0.1002 mL 0.5008 mL 1.0017 mL 2.5041 mL
30 mM 0.0835 mL 0.4174 mL 0.8347 mL 2.0868 mL
40 mM 0.0626 mL 0.3130 mL 0.6260 mL 1.5651 mL
50 mM 0.0501 mL 0.2504 mL 0.5008 mL 1.2521 mL
60 mM 0.0417 mL 0.2087 mL 0.4174 mL 1.0434 mL
80 mM 0.0313 mL 0.1565 mL 0.3130 mL 0.7825 mL
100 mM 0.0250 mL 0.1252 mL 0.2504 mL 0.6260 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Lenumlostat 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:

Lenumlostat2007885-39-2PAT-1251 GB2064PAT1251PAT 1251GB2064GB 2064GB-2064Monoamine OxidaseMAOInhibitorinhibitorinhibit

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