| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
UK-370106 (Compound 7) has a potency of 2.3 µM to inhibit MMP-13, which is roughly 100 times lower than its potency to inhibit MMP-3. The zinc metalloproteases PCP and TACE were found to be inactive against UK-370106 (IC50 > 100 µM). Additionally, MMP-2 (IC50 of 34.2 µM), MMP-7 (IC50 of 5.8 µM), and MMP-8 Potency (IC50 of 1.75 µM), MMP-9 (IC50 of 30.4 µM), and MMP-14 (IC50 of 66.9 µM) were all inhibited [1]. Up to the highest dose tested (100 µM), UK-370106 potently inhibits [3H]-fibronectin cleavage by MMP-3 (IC50 of 320 nM), but not [3H]-gelatin cleavage by MMP-2 or -9[1]. At concentrations of 50–100 µM in vitro, UK-370106 is not cytotoxic to fibroblasts, keratinocytes, or endothelial cells and has no effect on their proliferation [1].
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|---|---|
| ln Vivo |
UK-370106 (compound 7) was removed from cutaneous tissue slowly (t1/2 = 3 days) but quickly (t1/2 = 23 min) from plasma. Topical treatment of UK-370106 for 6 days effectively suppressed MMP-3 in vitro in a chronic skin ulcer model [1].
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| References |
| Molecular Formula |
C₃₅H₄₄N₂O₅
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|---|---|
| Molecular Weight |
572.73
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| Exact Mass |
572.325
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| CAS # |
230961-21-4
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| PubChem CID |
9808181
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| Appearance |
White to off-white solid powder
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| Density |
1.123g/cm3
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| Boiling Point |
802.689ºC at 760 mmHg
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| Flash Point |
439.25ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.56
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| LogP |
6.892
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
42
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| Complexity |
843
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| Defined Atom Stereocenter Count |
3
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| SMILES |
CC1=C(C=CC(=C1)CCC[C@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](COC)C2=CC=CC=C2)C(C)(C)C)C3=CC=CC=C3
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| InChi Key |
NSMABJUGSNPHMN-BHYWQNONSA-N
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| InChi Code |
InChI=1S/C35H44N2O5/c1-24-21-25(19-20-29(24)26-14-8-6-9-15-26)13-12-18-28(22-31(38)39)33(40)37-32(35(2,3)4)34(41)36-30(23-42-5)27-16-10-7-11-17-27/h6-11,14-17,19-21,28,30,32H,12-13,18,22-23H2,1-5H3,(H,36,41)(H,37,40)(H,38,39)/t28-,30-,32-/m1/s1
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| 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
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| Synonyms |
UK370106 UK 370106
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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 : ~200 mg/mL (~349.20 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.73 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 50.0 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: ≥ 5 mg/mL (8.73 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 50.0 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: ≥ 5 mg/mL (8.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7460 mL | 8.7301 mL | 17.4602 mL | |
| 5 mM | 0.3492 mL | 1.7460 mL | 3.4920 mL | |
| 10 mM | 0.1746 mL | 0.8730 mL | 1.7460 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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