1. Neuronal Signaling
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  3. PXS-5505

PXS-5505  (Synonyms: LOX-IN-3 dihydrochloride monohydrate)

製品番号: HY-138625B
取扱説明書 Technical Support

PXS-5505 (LOX-IN-3 dihydrochloride monohydrate) (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor. PXS-5505 can be used for fibrosis, cancer and angiogenesis research.

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PXS-5505

PXS-5505 構造式

CAS 番号 : 2414974-55-1

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製品説明

PXS-5505 (LOX-IN-3 dihydrochloride monohydrate) (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor. PXS-5505 can be used for fibrosis, cancer and angiogenesis research[1].

IC50 & Target

IC50: <1 μM (human LOXL2), <10 μM (bovine LOX)[1]

体外実験

PXS-5505 (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50 values of <10 μM and <1 μM, respectively[1].
PXS-5505 exhibits sustained inhibition of LOXL1 and LOXL2[1].
PXS-5505 is less active against SSAO/VAP-1 and MAO-B activities[1].

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

体内実験

PXS-5505 (LOX-IN-3 dihydrochloride monohydrate) (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1].
PXS-5505 (LOX-IN-3 dihydrochloride monohydrate) (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1].
PXS-5505 (LOX-IN-3 dihydrochloride monohydrate) (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1].

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

Animal Model: Male Wistar rats[1]
Dosage: 30 mg/kg
Administration: Oral administration, single dose
Result: Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta).
Animal Model: Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage, daily for 14 days
Result: Increased kidney weight and thickness and reduced the area of fibrosis.
Animal Model: C57Bl/6 mice, Bleomycin-induced lung fibrosis model
Dosage: 15 mg/kg
Administration: Oral gavage, daily for 21 days
Result: Significantly reduced the Ashcroft score and the lung weight.
臨床実験
分子量

371.26

分子式

C13H17Cl2FN2O3S

CAS 番号
SMILES

NC/C=C(F)/CS(=O)(C1=CC=CC2=C1N=CC=C2)=O.Cl.O.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

純度とドキュメンテーション
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製品名:
PXS-5505
製品番号:
HY-138625B
数量:
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