UK 383367

UK-383367 is a procollagen C-proteinase (BMP-1) inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.

UK 383367 Chemical Structure

UK 383367 Chemical Structure

CAS No. 348622-88-8

Purity & Quality Control

UK 383367 Related Products

Biological Activity

Description UK-383367 is a procollagen C-proteinase (BMP-1) inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs.
Targets
Procollagen C proteinase [1]
44 nM
In vitro
In vitro UK-383367 is effective at penetrating human skin. [1] 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. [2] UK-383367 is a weakly acidic compound and lipophilic. [3]
In Vivo
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%. [3]
Animal Research Animal Models Sprague–Dawley rats
Dosages 2 mg/kg
Administration Intravenously

Chemical Information & Solubility

Molecular Weight 324.38 Formula

C15H24N4O4

CAS No. 348622-88-8 SDF Download UK 383367 SDF
Smiles C1CCC(CC1)CCCC(CC(=O)NO)C2=NC(=NO2)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (200.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 65 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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