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PXS-5153A monohydrochloride

Catalog No. T12585L CAS 2125956-82-1

Synonyms: PXS-5153A monohydrochloride (2125956-82-1 free base)

PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis

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PXS-5153A monohydrochloride Chemical Structure

PXS-5153A monohydrochloride, CAS 2125956-82-1

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 987.00
50 mg	10-14 weeks	$ 1,360.00
100 mg	10-14 weeks	$ 1,860.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

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Description	PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride dose-dependently reduced LOXL2-mediated collagen oxidation and collagen crosslinking in vitro which may represent an innovative therapeutic approach for the treatment of fibrosis
In vitro	PXS-5153A demonstrates potent inhibition of LOXL2 across various mammalian species, with an IC50 value of less than 40 nM. It also effectively inhibits human LOXL3, having an IC50 of 63 nM. This compound exhibits significant selectivity, being more than 40-fold more selective for LOXL2 over LOX and LOXL1, and exhibits over 700-fold selectivity against other related amine oxidases. Additionally, PXS-5153A acts rapidly, nearly completely inhibiting enzymatic activity within 15 minutes [1].
In vivo	As expected, rhLOXL2 induces collagen oxidation in a dose-dependent manner while PXS-5153A impedes collagen oxidation in a dose-dependent manner. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl 4 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 CCl 4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl 4 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].

Synonyms	PXS-5153A monohydrochloride (2125956-82-1 free base)
Molecular Weight	475.41
Formula	C20H25Cl2FN4O2S
CAS No.	2125956-82-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (569.54 mM), Sonication is recommended.

References and Literature

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.

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Keywords

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