2. Neuronal Signaling
  3. Monoamine Oxidase
  4. PXS-5120A

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).

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PXS-5120A Chemical Structure

PXS-5120A Chemical Structure

CAS No. : 2125955-70-4

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5 mg USD 620 In-stock
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Based on 1 publication(s) in Google Scholar

PXS-5120A Related Antibodies

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Description

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1].

IC50 & Target

pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like); Ki: 83 nM (Lysyl Oxidase-like 2)[1]
In Vitro

PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.

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

PXS-5120A Related Antibodies
In Vivo

PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout[1].

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

481.97

Formula

C22H25ClFN3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC2=C(N(C/C(F)=C/CN)C(C)=C2C3=CC=CC(S(=O)(N(C)C)=O)=C3)C=C1)O.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (259.35 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 2.0748 mL 10.3741 mL 20.7482 mL
5 mM 0.4150 mL 2.0748 mL 4.1496 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 (sealed storage, away from moisture). 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 (sealed storage, away from moisture). 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 2.0748 mL 10.3741 mL 20.7482 mL 51.8704 mL
5 mM 0.4150 mL 2.0748 mL 4.1496 mL 10.3741 mL
10 mM 0.2075 mL 1.0374 mL 2.0748 mL 5.1870 mL
15 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4580 mL
20 mM 0.1037 mL 0.5187 mL 1.0374 mL 2.5935 mL
25 mM 0.0830 mL 0.4150 mL 0.8299 mL 2.0748 mL
30 mM 0.0692 mL 0.3458 mL 0.6916 mL 1.7290 mL
40 mM 0.0519 mL 0.2594 mL 0.5187 mL 1.2968 mL
50 mM 0.0415 mL 0.2075 mL 0.4150 mL 1.0374 mL
60 mM 0.0346 mL 0.1729 mL 0.3458 mL 0.8645 mL
80 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6484 mL
100 mM 0.0207 mL 0.1037 mL 0.2075 mL 0.5187 mL
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PXS-5120A 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:

PXS-5120A2125955-70-4Monoamine OxidaseMAOInhibitorinhibitorinhibit

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