XL-784 free base
- CAS No.
- 1356992-21-6
- Chemical Name:
- XL-784 free base
- Synonyms
- XL-784 free base;XL784 free base,XL 784 free base;1-Piperazinecarboxylic acid, 4-[[4-(4-chlorophenoxy)-3,5-difluorophenyl]sulfonyl]-3-[(hydroxyamino)carbonyl]-, 2-methoxyethyl ester
- CBNumber:
- CB85821460
- Molecular Formula:
- C21H22ClF2N3O8S
- Molecular Weight:
- 549.93
- MDL Number:
- MFCD32641626
- MOL File:
- 1356992-21-6.mol
XL-784 free base Chemical Properties,Uses,Production
Description
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with 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 is a highly potent, low-molecular-weight (1,122 g/mol) inhibitor of MMPs that has very limited aqueous solubility (20 μg/mL). XL-784 potently inhibits MMP-2, MMP-13, andADAM10 [TNF-α-converting enzyme (TACE)] activity in vitro, with 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, it exhibits low potency for inhibition of MMP-1 (IC50 ~2,000 nM)[1].
All mice tolerate the treatments similarly. Control mice all developed aneurysms with a mean %△AD of 158.5%±4.3%. 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 highest 2 doses of XL-784 tested are more effective than doxycycline (112.2%±2.0%, P<0.05) in inhibiting maximal dilatation of the aorta after elastase perfusion[2].
References
[1]. Williams JM, et al. Evaluation of metalloprotease inhibitors on hypertension and diabetic nephropathy. Am J Physiol Renal Physiol. 2011 Apr;300(4):F983-98. [2]. Ennis T, et al. Effect of novel limited-spectrum MMP inhibitor XL784 in abdominal aortic aneurysms. J Cardiovasc Pharmacol Ther. 2012 Dec;17(4):417-26.
XL-784 free base Preparation Products And Raw materials
Raw materials
Preparation Products
XL-784 free base Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19696 | 58 |
Supplier | Advantage |
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TargetMol Chemicals Inc. | 58 |
TargetMol Chemicals Inc. | 58 |