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Cat. No.: HY-114286

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PXS-5153A

Name: PXS-5153A
Brand: MedChemExpress
SKU: HY-114286
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1 Cited Publications

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Based on 1 publication(s) in Google Scholar

PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC₅₀ of <40 nM for LOXL2 across all mammalian species and an IC₅₀ of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

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CAS No.: 2125956-82-1
Formule: C₂₀H₂₅Cl₂FN₄O₂S
Masse moléculaire:475.41

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (278 KB)

PXS-5153A Chemical Structure

CAS No.: 2125956-82-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
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Activité biologique

Description

IC₅₀ & Target

IC50: <40 nM (LOXL2 across all mammalian species), 63 nM (human LOXL3)^[1].

Voir tous les produits spécifiques à Isoform Monoamine Oxidase :

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In Vitro

PXS-5153A exhibits an IC₅₀ of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC₅₀ value of 63 nM. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes ^[1].

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

In Vivo

As expected, rhLOXL2 dose-dependently induce oxidation of collagen with PXS-5153A dose-dependently impeding collagen oxidation. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl₄ treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation compared to the CCl₄ treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl₄ group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A^[1].

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

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Chemical Information

CAS No. 2125956-82-1
Masse moléculaire 475.41
Formule C₂₀H₂₅Cl₂FN₄O₂S
SMILES

CC(N1C/C(F)=C/CN)=C(C2=CC=CC(S(N(C)C)(=O)=O)=C2)C3=C1C=CC=N3.Cl.Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Neuron

Single-cell dissection of the human blood-brain barrier and glioma blood-tumor barrier. [Abstract]

2024 Sep 25;112(18):3089-3105.e7. PMID: 39191260

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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PXS-5153A

1 Cited Publications

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Pureté et documentation
Références

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PXS-5153A

Publications Citing Use of MedChemExpress (MCE) PXS-5153A

Voir tous les produits spécifiques à Isoform Monoamine Oxidase