PAT-1251( PAT 1251 | PAT1251 )

Catalog No. M13132 CAS No. 2007885-39-2

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Datasheet

HNMR

HPLC

MSDS

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Product Name

PAT-1251
Note

Research use only, not for human use.
Brief Description

PAT-1251 (PAT 1251, PAT1251) is a?potent, selective and orally bioavailable lysyl oxidase-like 2 (LOXL2) inhibitor with IC50 of 0.71 uM in human whole blood assays.
Description

PAT-1251 (PAT 1251, PAT1251) is a?potent, selective and orally bioavailable lysyl oxidase-like 2 (LOXL2) inhibitor with IC50 of 0.71 uM in human whole blood assays, with high selectivity over LOX (400-fold) and other amine oxidases; exhibits efficacy in mouse bleomycin lung fibrosis model.Fibrosis Phase 1 Clinical.
In Vitro

PAT-1251 is a Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 shows highly selective for LOXL2 over other key members of the amine oxidase family, such as the copper-dependent amine oxidases semicarbazide-sensitive amine oxidase (SSAO) and diamine oxidase (DAO), in addition to the flavin-dependent monoamine oxidases A (MAO-A) and B (MAO-B), with <10% inhibition at 10 μM.
In Vivo

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Synonyms

PAT 1251 | PAT1251
Pathway

Others
Target

Other Targets
Recptor

Other Targets
Research Area

Other Indications
Indication

Fibrosis

CAS Number

2007885-39-2
Formula Weight

399.346
Molecular Formula

C18H17F4N3O3
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 130 mg/mL 325.54 mM
SMILES

O=C(C1=CC=CC(OC2=NC(C(F)(F)F)=CC(CN)=C2)=C1)N3C[C@@H](F)[C@H](O)C3
Chemical Name

(3-((4-(aminomethyl)-6-(trifluoromethyl)pyridin-2-yl)oxy)phenyl)((3R,4R)-3-fluoro-4-hydroxypyrrolidin-1-yl)methanone

1. Rowbottom MW, et al. J Med Chem. 2017 May 25;60(10):4403-4423.

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