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XL-784 free base

Catalog No. T13357Cas No. 1356992-21-6

XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP) with IC50 values of ~1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively.

XL-784 free base

XL-784 free base

Catalog No. T13357Cas No. 1356992-21-6
XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP) with IC50 values of ~1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively.
Pack SizePriceAvailabilityQuantity
25 mg$2,1208-10 weeks
50 mg$2,7808-10 weeks
100 mg$3,7008-10 weeks
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Product Introduction

Bioactivity
Description
XL-784 free base is a selective inhibitor of matrix metalloproteinases (MMP) with IC50 values of ~1900, 0.81, 120, 10.8, 18, and 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, and MMP-13, respectively.
Targets&IC50
MMP3:120 nM, MMP8:10.8 nM, MMP2:0.81 nM, MMP1:1900 nM, MMP13:0.56 nM, MMP9:18 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%). The 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 Weight549.93
FormulaC21H22ClF2N3O8S
Cas No.1356992-21-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 250 mg/mL (454.60 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8184 mL9.0921 mL18.1841 mL90.9207 mL
5 mM0.3637 mL1.8184 mL3.6368 mL18.1841 mL
10 mM0.1818 mL0.9092 mL1.8184 mL9.0921 mL
20 mM0.0909 mL0.4546 mL0.9092 mL4.5460 mL
50 mM0.0364 mL0.1818 mL0.3637 mL1.8184 mL
100 mM0.0182 mL0.0909 mL0.1818 mL0.9092 mL

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