MDL 101146

Names

[ Name ]:
MDL 101146

[Synonym ]:
N-[4-(4-morpholinylcarbonyl)benzoyl]-L-valyl-N-[3,3,4,4,4-pentafluoro-1-(1-methylethyl)-2-oxobutyl]-L-prolinamide
(S)-1-{(S)-3-Methyl-2-[4-(morpholine-4-carbonyl)-benzoylamino]-butyryl}-pyrrolidine-2-carboxylic acid (3,3,4,4,4-pentafluoro-1-isopropyl-2-oxo-butyl)-amide
[4-(4-morpholinylcarbonyl)benzoyl]Val-Pro-L,D-Val pentafluoroethylketone

Biological Activity

[Description]:

MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis[1][2].

[Related Catalog]:

Research Areas >> Infection

Signaling Pathways >> Metabolic Enzyme/Protease >> Elastase

Research Areas >> Inflammation/Immunology

[Target]

Ki for neutrophil elastase: 25 nM (human); 18 nM (rat)[1][2]

[In Vitro]

MDL 101,146 inhibits human neutrophil elastase with a Ki value of 25 nM[1]. MDL 101,146 inhibits rat neutrophil elastase activity in a dose-related manner with a Ki value of 18 nM[2].

[In Vivo]

MDL 101146 (oral, 200 mg/kg/day) significantly inhibits swelling and joint destruction in collagen-induced arthritis but not in adjuvant arthritis[2]. Animal Model: Rats[2] Dosage: 200 mg/kg Administration: Oral, 200 mg/kg/day Result: Inhibited the severity of collagen-induced arthritis. Had a bone and cartilage sparing effect in the tibio-tarsal joint of animals with collagen-induced arthritis.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₇F₅N₄O₆

[ Molecular Weight ]:
632.61900

[ Exact Mass ]:
632.26300

[ PSA ]:
125.12000

[ LogP ]:
3.46950

Related Compounds

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