PXS-5153A

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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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PXS-5153A monohydrochloride) usually boasts enhanced water solubility and stability.

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

PXS-5153A Chemical Structure

CAS No. : 2125956-82-1

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Other In-stock Forms of PXS-5153A:

PXS-5153A monohydrochloride

Other Forms of PXS-5153A:

PXS-5153A monohydrochloride In-stock

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Biological Activity
Protocol
Purity & Documentation
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Description	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.
IC₅₀ & Target	IC50: <40 nM (LOXL2 across all mammalian species), 63 nM (human LOXL3)^[1].
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. PXS-5153A Related Antibodies
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.
Molecular Weight	475.41
Formula	C₂₀H₂₅Cl₂FN₄O₂S
CAS No.	2125956-82-1
SMILES	CC(N1C/C(F)=C/CN)=C(C2=CC=CC(S(N(C)C)(=O)=O)=C2)C3=C1C=CC=N3.Cl.Cl
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (278 KB) Handling Instructions (2659 KB)
References	[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]

Animal Administration
^[1]

Rats^[1]
Sprague Dawley rats are orally administered with 0.25 μL/g Carbon tetrachloride (CCl₄) in olive oil solution, starting from day 0, 3 times per week for 6 weeks. PXS-5153A is given by oral gavage after 3 weeks of CCl₄ administration and continued throughout the remainder of the study at 3 mg/kg (low dose) or 10 mg/kg (high dose) once a day or 10 mg/kg (high dose) three times a week. Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels were assessed in the plasma.
Mice
NASH is established in male C57/BL6 mice by a single subcutaneous injection of 200 μg streptozotocin after birth and with a high fat diet ad libitum after 4 weeks of age (day 28 ± 2) until 14 weeks of age. Mice are orally administered with 10 mg/kg PXS-5153A once daily from 8 to 14 weeks of age. ALT levels are assessed in the plasma.
Mice
Myocardial infarction (MI) is induced in C57/BL6 mice by occluding the left coronary artery. At 24 hours post-surgery, animals receive echocardiography. Infarcted mice with high cardiac function (FS > 40%) or low cardiac function (FS<10%) are excluded from the study. The remaining mice are treated q.d., p.o., with 25 mg/kg of PXS-5153A for 4 weeks. At the end of the experiment, echocardiography is performed on mice to assess left ventricular function and remodelling, followed by heart collection. The heart is fixed with 10% formalin. Fibrosis is assessed in the non-infarct area^[1].

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

References

[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]

PXS-5153A Related Classifications

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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-5153A2125956-82-1Monoamine OxidaseMAOInhibitorinhibitorinhibit

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