3-(Aminocarbonyl)-β-(3-cyclohexylpropyl)-N-hydroxy-1,2,4-oxadiazole-5-propanamide Chemical Properties

Melting point:

136-138℃

Density 

1.233

storage temp. 

Sealed in dry,Room Temperature

solubility 

DMSO: >30mg/mL

form 

powder

pka

9.03±0.20(Predicted)

color 

white to off-white

optical activity

[α]/D ≥15°, c = 0.5 in methanol

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

3-(Aminocarbonyl)-β-(3-cyclohexylpropyl)-N-hydroxy-1,2,4-oxadiazole-5-propanamide Usage And Synthesis

Uses

Potent and selective nonpeptidic inhibitor of procollagen C-proteinase (PCP) inhibitor. A potential dermal anti-scarring agent.

Biological Activity

uk 383367 is a novel procollagen c-protein (pcp) inhibitor being investigated for the treatment of post-surgical dermal scarring, which potently inhibits the activity of pcp with the value of 50% inhibition concentration ic50 of 44 nm, as well as a selective inhibitor of matrix metalloproteinases (mmps) with values of ic50 >60,000 nm for mmp-2 and >10,000 nm for mmp-1, mmp-3, mmp-9 and mmp-4. although the mechanism is not clear yet, uk 383367 also exhibits weak inhibitory effects against phosphodiesterase-4 (pde-4) enzyme, including pde-4a, pde-4b, pde-4c and pde-4d, with values of ic50 of 1.8 μm, 1.5 μm, 2.4 μm and 0.9 μm respectively.g. a. allan, j. i. gedge, a. n. r. nedderman, s. j. roffey, h. f. small and r. webster. pharmacokinetics and metabolism of uk-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. xenobiotica 2006; 36(5): 399-418bailey s, fish pv, billotte s, bordner j, greiling d, james k, mcelroy a, mills je, reed c, webster r.ff. succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen c-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. bioorg med chem lett. 2008;18(24):6562-6567

storage

Store at -20°C

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