UK-383367

SKU: orb1689388

Description

UK-383367 is a potent and selective inhibitor of procollagen C-proteinase (PCP, also known as BMP-1), exhibiting an IC50 of 44 nM with excellent selectivity over matrix metalloproteinases (MMPs). This small molecule is a valuable research tool for investigating collagen biosynthesis and fibrotic processes in both cellular and animal models of fibrosis.

Research Area

Metabolism Research

Key Properties

• CAS Number: 348622-88-8
• MW: 324.38
• Purity: >99.99% (May vary between batches)
• Formula: C₁₅H₂₄N₄O₄
• SMILES: NC(=O)c1noc(n1)[C@H](CCCC1CCCCC1)CC(=O)NO
• Target: Procollagen C Proteinase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.17 mM);Ethanol:65 mg/mL (200.38 mM);DMSO:65 mg/mL (200.38 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  Procollagen C proteinase:44 nM
• In Vivo:
  Plasma protein binding values for UK-383367 in rat, dog and human are 95%, 93% and 94%, respectively. UK-383367 following incubation in rat plasma results in the half-life of 49 min. UK-383367 following single intravenous administration (2 mg/kg) to rat results in the plasma clearance of 157 mL min 1 kg 1, the volume of distribution of 12 L kg 1, and an elimination half-life of 0.8 hour. UK-383367 following single intravenous administration (0.5 mg/kg) to dog results in the plasma clearance of 35 mL min 1 kg 1, the volume of distribution of 4.6 L kg 1, and an elimination half-life of 1.5 hours. UK-383367 following oral administration (2 mg/kg) to dog results in Cmax of 110 ng/mL, Tmax of 0.5-1.5 hour and oral bioavilability of 13%.
• In Vitro:
  UK-383367 is effective at penetrating human skin. UK-383367 inhibits collagen deposition with IC50 of ~2 μM. UK-383367 has modest affinity for all the PDE-4 subtypes PDE-4a, PDE-4b, PDE-4c and PDE-4d with IC50 of 1.8 μM, 1.5 μM, 2.4 μM and 0.9 μM, respectively. UK-383367 is a weakly acidic compound and lipophilic.

Storage & Handling

• Storage: keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Procollagen C proteinase, Procollagen C Proteinase, ProcollagenCProteinase, UK 383367, UK383367, UK-383367

Compound Identifiers

PubChem CID

9818682