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UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $775 | 35 days |
Description | UK-370106 is a potent and highly selective inhibitor of MMP-3 (IC50: 23 nM) and MMP-12 (IC50: 42 nM), effectively inhibiting the cleavage of [3H]-fibronectin by MMP-3 (IC50: 320 nM). |
Targets&IC50 | MMP7:5.8 μM, MMP2:34.2 μM, MMP13:2.3 μM, MMP9:30.4 μM, MMP12:42 nM, MMP8:1.75 μM, MMP14:66.9 μM, MMP3:23 nM |
In vitro | UK-370106 potency 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)[1]. |
In vivo | Following intravenous (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is rapidly cleared from plasma (t1/2 = 23 min) but slowly from dermal tissue (t1/2 approximately 3 days). Topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo in a model of chronic dermal ulcers [1]. |
Molecular Weight | 572.73 |
Formula | C35H44N2O5 |
Cas No. | 230961-21-4 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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