UK 370106 |
| رقم الكتالوجGC16579 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 230961-21-4
Sample solution is provided at 25 µL, 10mM.
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IC50: 23 nm (MMP-3)
Stromelysin-1 also known as matrix metalloproteinase-3 (MMP-3) is an enzyme that in humans is encoded by the MMP3 gene. Proteins of the matrix metalloproteinase (MMP) family are involved in the breakdown of extracellular matrix and during tissue remodeling in normal physiological processes, such as embryonic development and reproduction, as well as in disease processes, such as arthritis, and tumour metastasis (http://en.wikipedia.org/wiki/MMP-3).
In vitro: UK-370106, a potent inhibitor of MMP-3 (IC50 ) 23 nM) with >1200-fold weaker potency vs MMP-1, -2, -9, and -14. MMP-13, may contribute to the pathology of chronic wounds. UK-370106 potently inhibited cleavage of [3H]-fibronectin by MMP-3 (IC50 ) 320 nM) but not cleavage of [3H]-gelatin by either MMP-2 or -9 (up to 100 íM). UK-370106 had little effect, at MMP-3 selective concentrations, on keratinocyte migration over a collagen matrix in vitro, which is a model of the re-epithelialization process [1].
In vivo: Following iv (rat) or topical administration to dermal wounds (rabbit), UK-370106 was cleared rapidly (t1/2=23 min) from plasma, but slowly (t1/2 ~ 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibited MMP-3 ex vivo. These data suggest UK-370106 is sufficiently potent to inhibit MMP-3-mediated matrix degradation while leaving unaffected cellular migration mediated by MMPs 1, 2, and 9. These properties make UK-370106 a suitable candidate for progression to clinical trials in human chronic dermal wounds, such as venous ulcers [1].
Clinical trial: Pfizer described the discovery of UK-370106, a highly selective peptidicMMP-3 inhibitor, which was identified as a clinical candidate for the topical treatment of chronic dermal ulcers [2], however, it is now still in the preclinical stage and no clinical trial is ongoing.
References:
[1] Fray MJ, Dickinson RP, Huggins JP, Occleston NL. A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003;46(16):3514-25.
[2] Whitlock GA, Dack KN, Dickinson RP, Lewis ML. A novel series of highly selective inhibitors of MMP-3. Bioorg Med Chem Lett. 2007;17(24):6750-3.
| Cas No. | 230961-21-4 | SDF | |
| Chemical Name | (3R)-3-[[(2S)-1-[[(1S)-2-methoxy-1-phenylethyl]amino]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]-6-(3-methyl-4-phenylphenyl)hexanoic acid | ||
| Canonical SMILES | CC1=C(C=CC(=C1)CCCC(CC(=O)O)C(=O)NC(C(=O)NC(COC)C2=CC=CC=C2)C(C)(C)C)C3=CC=CC=C3 | ||
| Formula | C35H44N2O5 | M.Wt | 572.73 |
| الذوبان | <57.27mg/ml in DMSO; <14.32mg/ml in ethanol | Storage | Store at 4°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.746 mL | 8.7301 mL | 17.4602 mL |
| 5 mM | 349.2 μL | 1.746 mL | 3.492 mL |
| 10 mM | 174.6 μL | 873 μL | 1.746 mL |
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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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