| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
UK-383367 targets bone morphogenetic protein 1 (BMP-1), a metalloproteinase that is also known as procollagen C-proteinase (PCP). BMP-1 is a member of the astacin family of zinc-dependent metalloproteinases and plays an essential role in extracellular matrix formation by cleaving the C-terminal propeptides of procollagens I, II, and III. This proteolytic cleavage is a critical step in the assembly of mature collagen fibrils, which are the major structural components of the extracellular matrix. By inhibiting BMP-1/PCP, UK-383367 prevents the formation of mature collagen fibrils and reduces collagen deposition. The compound also shows modest affinity for all four PDE-4 subtypes. Its selectivity for BMP-1 over other matrix metalloproteinases is greater than 200-fold.
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| ln Vitro |
In vitro, UK-383367 is a potent inhibitor of BMP-1/procollagen C-proteinase with an IC50 of 44 nM. The compound inhibits collagen deposition with an IC50 of approximately 2 μM. It also shows modest affinity for all four PDE-4 subtypes, with IC50 values of 1.8 μM (PDE-4a), 1.5 μM (PDE-4b), 2.4 μM (PDE-4c), and 0.9 μM (PDE-4d). UK-383367 is more than 200-fold selective for BMP-1 over a panel of matrix metalloproteinases, confirming its specificity for the intended target. The compound's ability to inhibit collagen deposition has been demonstrated in cell-based assays.
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| ln Vivo |
In vivo, UK-383367 has demonstrated dermal anti-scarring activity. By inhibiting BMP-1 and reducing collagen deposition, the compound has the potential to prevent or reduce scar formation following injury. The compound has been investigated for its potential applications in fibrosis and other conditions characterized by excessive collagen deposition. Its oral bioavailability and selectivity for BMP-1 make it a promising candidate for further evaluation in preclinical models of fibrosis and scarring.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for UK-383367 involve measuring the enzymatic activity of BMP-1/procollagen C-proteinase using fluorogenic or chromogenic peptide substrates. The enzyme is incubated with a synthetic peptide substrate (e.g., a fluorogenic peptide containing the cleavage site of procollagen) and varying concentrations of UK-383367. The rate of substrate cleavage is monitored fluorometrically or spectrophotometrically, and IC50 values are calculated from inhibition curves. Selectivity profiling against a panel of matrix metalloproteinases and other proteases is performed to confirm the compound's specificity for BMP-1. PDE-4 inhibition assays are also performed using purified PDE-4 subtypes.
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| Cell Assay |
In vitro cell-based experiments for UK-383367 are conducted using fibroblasts or other collagen-producing cells. Cells are cultured and treated with UK-383367 at varying concentrations. Collagen deposition is assessed by measuring collagen protein levels (e.g., by Western blot or ELISA) or by using radioactive proline incorporation assays. The compound's effects on cell viability, proliferation, and extracellular matrix protein expression are evaluated. Inhibition of collagen deposition with an IC50 of approximately 2 μM has been demonstrated in these assays.
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| Animal Protocol |
In vivo animal experiments for UK-383367 are performed in animal models of fibrosis, scarring, and wound healing. The compound is administered orally or topically, and its effects on collagen deposition, scar formation, and tissue remodeling are assessed. In models of dermal scarring, the compound's ability to reduce scar volume and improve tissue architecture is evaluated. Histological analysis of skin tissue, measurement of collagen content (e.g., hydroxyproline assay), and assessment of wound healing parameters are performed to evaluate efficacy.
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| ADME/Pharmacokinetics |
UK-383367 is a small molecule (MW 324.38) with good oral bioavailability and systemic exposure. The compound's physicochemical properties support its use in in vivo studies. Detailed pharmacokinetic parameters, including Cmax, Tmax, AUC, and half-life, are available from preclinical studies. Its oral bioavailability and selectivity for BMP-1 make it suitable for evaluation in animal models of fibrosis and scarring.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies have been conducted to evaluate the safety profile of UK-383367. The compound is well-tolerated at efficacious doses in animal models, with no significant off-target toxicity reported in available literature. Its selectivity for BMP-1 over other matrix metalloproteinases (>200-fold) suggests a favorable safety profile with minimal off-target effects. However, as with any compound that modulates extracellular matrix remodeling, potential effects on normal tissue homeostasis should be considered.
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| References |
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| Additional Infomation |
UK-383367 is also known as UK 383367. It is a research compound used primarily for studying the role of BMP-1/procollagen C-proteinase in collagen biosynthesis, extracellular matrix remodeling, fibrosis, and scarring. The compound has not been approved for clinical use and remains an investigational agent for research purposes only. Its potent and selective inhibition of BMP-1 makes it a valuable tool for exploring new therapeutic approaches for fibrotic diseases and scar prevention.
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| Molecular Formula |
C15H24N4O4
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|---|---|
| Molecular Weight |
C15H24N4O4
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| Exact Mass |
324.179
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| CAS # |
348622-88-8
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| PubChem CID |
9818682
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Melting Point |
136-138℃
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| Index of Refraction |
1.541
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| LogP |
1.37
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
401
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1CCC(CC1)CCC[C@H](CC(=O)NO)C2=NC(=NO2)C(=O)N
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| InChi Key |
ARJCBSRIPGJMAD-LLVKDONJSA-N
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| InChi Code |
InChI=1S/C15H24N4O4/c16-13(21)14-17-15(23-19-14)11(9-12(20)18-22)8-4-7-10-5-2-1-3-6-10/h10-11,22H,1-9H2,(H2,16,21)(H,18,20)/t11-/m1/s1
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| Chemical Name |
5-[(3R)-6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl]-1,2,4-oxadiazole-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~65 mg/mL (~200.38 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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