| Name | XL-784 free base |
| 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. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (6 mM), Sonication is recommended.
DMSO : 250 mg/mL (454.6 mM), Sonication is recommended.
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| Keywords | XL-784 free base | XL784 free base | XL-784 | XL784 | XL 784 free base | XL 784 | MMP-9 | MMP-8 | MMP-3 | MMP-2 | MMP-13 | MMP-1 |
| Inhibitors Related | Rhamnose monohydrate | Doxycycline (hyclate) | Chondroitin sulfate | Astragaloside IV | Doxycycline | Edaravone | Glucosamine | Anethole | Meloxicam | Chloramphenicol | Propoxur | Methylchloroisothiazolinone/Methylisothiazolinone Mixture |
United States
