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XL-784

Catalog No. T13358Cas No. 1224964-36-6

XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).

XL-784

XL-784

Catalog No. T13358Cas No. 1224964-36-6
XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
Pack SizePriceAvailabilityQuantity
2 mg$1985 days
5 mg$3325 days
25 mg$9878-10 weeks
50 mg$1,3608-10 weeks
100 mg$1,9908-10 weeks
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Product Introduction

Bioactivity
Description
XL-784 is a selective inhibitor of matrix metalloproteinases (MMP)(IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively).
Targets&IC50
MMP1:1900 nM, MMP2:0.81 nM, MMP8:10.8 nM, MMP9:18 nM, MMP13:0.56 nM, MMP3:120 nM
In vitro
XL-784 is a low-molecular-weight (1,122 g/mol) MMPs inhibitor. XL-784 potently inhibits MMP-2, MMP-13, and ADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro(IC50 values in the range of 1-2 nM). XL-784 also inhibits MMP-9 (IC50 ~20 nM) activity and ADAM17 (IC50 ~70 nM) also known as TACE. However, XL-784 exhibits low potency for inhibition of MMP-1 (IC50 ~2,000 nM)[1].
In vivo
Treatment with all doses of XL-784 and doxycycline are effective in inhibiting aortic dilatation. There is a clear dose-response relationship between XL-784 and reductions in aortic dilatation at harvest (50 mg/kg 140.4% ±3.2%; 125 mg/kg 129.3% ±5.1%; 250 mg/kg 119.2%±3.5%; all Ps<0.01 compared to control). This continues with the higher doses (375 mg/kg 88.6%±4.4%; 500 mg/kg 76.0%±3.5%). he two doses of the highest dose of XL-784 tested were more effective than doxycycline in inhibiting the maximum expansion of the aorta after elastase infusion (112.2%±2.0%, P<0.05) [2].
Chemical Properties
Molecular Weight1126.17
FormulaC42H46Cl2F4MgN6O16S2
Cas No.1224964-36-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 110 mg/mL (200.03 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM0.8880 mL4.4398 mL8.8797 mL44.3983 mL
5 mM0.1776 mL0.8880 mL1.7759 mL8.8797 mL
10 mM0.0888 mL0.4440 mL0.8880 mL4.4398 mL
20 mM0.0444 mL0.2220 mL0.4440 mL2.2199 mL
50 mM0.0178 mL0.0888 mL0.1776 mL0.8880 mL
100 mM0.0089 mL0.0444 mL0.0888 mL0.4440 mL

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