Ro 31-9790
Names
[ CAS No. ]:
145337-55-9
[ Name ]:
Ro 31-9790
[Synonym ]:
(2R)-N1-[(2S)-3,3-Dimethyl-1-(methylamino)-1-oxo-2-butanyl]-N4-hydroxy-2-isobutylsuccinamide
Butanediamide, N1-[(1S)-2,2-dimethyl-1-[(methylamino)carbonyl]propyl]-N4-hydroxy-2-(2-methylpropyl)-, (2R)-
Biological Activity
[Description]:
Ro 31-9790 is a synthetic metalloproteinase (MMP) inhibitor.
[Related Catalog]:
[Target]
MMP[1]
[In Vitro]
Ro 31-9790 inhibits L-selectin shedding from mouse and human lymphocytes, Jurkat T cells, and human monocytes with an IC50 of 0.3-0.4 μM on these cell types. The IC50 values obtained for Ro 31-9790 are 4.82 ± 0.75 μM, 1.16 ± 0.27 μM, 0.70 ± 0.06 μM, 4.47± 1.27 μM and 0.38 ± 0.05 μM for mouse lymphocyte L-selectin shedding, Jurkat L-selectin shedding, human lymphocyte L-selectin shedding, human monocyte L-selectin shedding and human monocyte TNF-α shedding[1].
[Cell Assay]
For mouse and human lymphocytes and Jurkat T cells, 100% inhibition is set as the percentage of cells positive for L-selectin in an untreated sample (after flow cytometric analysis) or the concentration of soluble L-selectin in the supernatant of an untreated cell sample (after ELISA); 0% inhibition is set at the appropriate value for a PMA-treated sample. For results from human monocytes, a different calculation is needed to allow direct comparison of L-selectin and TNF-α shedding. Therefore, in this case 100% inhibition is set as the percentage of cells positive for L-selectin in the presence of PMA+50 μM Ro 31-9790 or the percentage of cells positive for cell surface TNF-α in the presence of LPS+50 μM Ro 31-9790 (doses of Ro 31-9790 which gave maximal inhibition); 0% inhibition is set as the percentage of cells positive for L-selectin or TNF-α in the presence of PMA or LPS, respectively. Intermediate percent inhibition is calculated. The IC50 value for inhibitor in each system is defined as the concentration of inhibitor which gave 50% inhibition, where 100% inhibition is set as the percentage of cells positive for L-selectin or cell surface TNF-α in the presence of Phorbol myristate acetate (PMA)+50 μM Ro 31-9790 or Lipopolysaccharide (LPS)+50 μM Ro 31-9790, respectively (doses of Ro 31-9790 which gave maximal inhibition) and 0% inhibition is set as the percentage of cells positive for L-selectin or TNF-α in the presence of PMA or LPS alone, respectively[1].
[References]
[Related Small Molecules]
GM 6001
|
T-5224
|
SB-3CT
|
Batimastat
|
Astragaloside IV
|
Marimastat (BB-2516)
|
edaravone
|
TAPI-2
|
TAPI 1
|
ISOGINKGETIN
|
Arctigenin
|
CTS-1027
|
GI254023X
|
JNJ 0966
|
CL-82198
Chemical & Physical Properties
[ Density]:
1.1±0.1 g/cm3
[ Molecular Formula ]:
C15H29N3O4
[ Molecular Weight ]:
315.409
[ Exact Mass ]:
315.215820
[ LogP ]:
0.29
[ Index of Refraction ]:
1.484
[ Storage condition ]:
2-8℃