UK-370106
Based on 1 Customer Validation
UK-370106 is a potent and highly selective MMP-3 (IC50 of 23 nM) and MMP-12 (IC50 of 42 nM) inhibitor with >1200-fold higher potency than MMP-1, MMP-2, MMP-9, and MMP-14, and about 100-fold than MMP-13 and MMP-8. UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) and has little effect on keratinocyte migration in vitro.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 96.70%
- No. CAS: 230961-21-4
- Fòrmula: C35H44N2O5
- Peso molecular:572.73
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-130076
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CL-82198MMP-13 Inhibitor -
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ARP-100MMP-2 Inhibitor -
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CTS-1027MMP Inhibitor -
HY-107394
UK 356618MMP-3 Inhibitor -
HY-101535
ARP101MMP-2 Inhibitor -
HY-107428
PD-166793MMP Inhibitor
Actividad biológica
Descripciòn
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MMP-3 23 nM (IC50) |
MMP-12 42 nM (IC50) |
MMP-8 1.75 μM (IC50) |
MMP-13 2.3 μM (IC50) |
MMP-7 5.8 μM (IC50) |
MMP-9 30.4 μM (IC50) |
MMP-2 34.2 μM (IC50) |
MMP-14 66.9 μM (IC50) |
In Vitro
The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 μM, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC50 > 100 μM) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC50 of 34.2 μM), MMP-7 (IC50 of 5.8 μM), MMP-8 (IC50 of 1.75 μM), MMP-9 (IC50 of 30.4 μM) and MMP-14 (IC50 of 66.9 μM)[1].
UK-370106 potently inhibits cleavage of [3H]-fibronectin by MMP-3 (IC50 of 320 nM) but does not inhibit cleavage of [3H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 μM)[1].
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 μM in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 230961-21-4
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Appearance Solid
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Peso molecular 572.73
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Fòrmula C35H44N2O5
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Color White to off-white
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SMILES
CC1=C(C2=CC=CC=C2)C=CC(CCC[C@H](CC(O)=O)C(N[C@@H](C(C)(C)C)C(N[C@@H](C3=CC=CC=C3)COC)=O)=O)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 200 mg/mL (349.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.73 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Fray MJ, et al. A potent, selective inhibitor of matrix metalloproteinase-3 for the topical treatment of chronic dermal ulcers. J Med Chem. 2003 Jul 31;46(16):3514-25. [Content Brief]
[2]. Whitlock GA, et al. A novel series of highly selective inhibitors of MMP-3. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6750-3. Epub 2007 Oct 17. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7460 mL | 8.7301 mL | 17.4602 mL | 43.6506 mL |
| 5 mM | 0.3492 mL | 1.7460 mL | 3.4920 mL | 8.7301 mL | |
| 10 mM | 0.1746 mL | 0.8730 mL | 1.7460 mL | 4.3651 mL | |
| 15 mM | 0.1164 mL | 0.5820 mL | 1.1640 mL | 2.9100 mL | |
| 20 mM | 0.0873 mL | 0.4365 mL | 0.8730 mL | 2.1825 mL | |
| 25 mM | 0.0698 mL | 0.3492 mL | 0.6984 mL | 1.7460 mL | |
| 30 mM | 0.0582 mL | 0.2910 mL | 0.5820 mL | 1.4550 mL | |
| 40 mM | 0.0437 mL | 0.2183 mL | 0.4365 mL | 1.0913 mL | |
| 50 mM | 0.0349 mL | 0.1746 mL | 0.3492 mL | 0.8730 mL | |
| 60 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7275 mL | |
| 80 mM | 0.0218 mL | 0.1091 mL | 0.2183 mL | 0.5456 mL | |
| 100 mM | 0.0175 mL | 0.0873 mL | 0.1746 mL | 0.4365 mL |
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