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Technical Data
| Formula | C15H24N4O4 |
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| Molecular Weight | 324.38 | CAS No. | 348622-88-8 | |
| Solubility (25°C)* | In vitro | DMSO | 65 mg/mL (200.38 mM) | |
| Ethanol | 65 mg/mL (200.38 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | UK-383367 is a procollagen C-proteinase (BMP-1) inhibitor with IC50 of 44 nM, has excellent selectivity over MMPs. | ||
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| 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 | 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] |
Protocol (from reference)
| Animal Study:[3] |
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References
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Customer Product Validation
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Data from [Data independently produced by , , BMC Cancer, 2018, 18:508 ]
Selleck's UK 383367 has been cited by 6 publications
| Global Protease Activity Profiling Identifies HER2-Driven Proteolysis in Breast Cancer [ ACS Chem Biol, 2021, 10.1021/acschembio.0c01000] | PubMed: 33765766 |
| Poldip2 mediates blood-brain barrier disruption and cerebral edema by inducing AQP4 polarity loss in mouse bacterial meningitis model [ CNS Neurosci Ther, 2020, 10.1111/cns.13446] | PubMed: 32790044 |
| Extracellular BMP1 is the major proteinase for C-terminal proteolysis of type I procollagen in lung fibroblasts [ Am J Physiol Cell Physiol, 2020, 10.1152/ajpcell.00012.2020] | PubMed: 33206546 |
| [ Am J Physiol Renal Physiol, 2019, ] | PubMed: 31545926 |
| Clinical significance and biological role of cancer-derived Type I collagen in lung and esophageal cancers [ Thorac Cancer, 2019, 10(2):277-288] | PubMed: 30604926 |
| Upregulation of bone morphogenetic protein 1 is associated with poor prognosis of late-stage gastric Cancer patients [Hsieh YY, et al. BMC Cancer, 2018, 18(1):508] | PubMed: 29720137 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.