Company Name: |
TargetMol Chemicals Inc.
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Tel: |
4008200310 |
Email: |
marketing@tsbiochem.com |
Products Intro: |
Product Name:XL-784 free base;XL784 free base,XL 784 free base CAS:1356992-21-6 Purity:98% Package:5 mg
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| XL-784 free base Basic information |
Product 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 | CAS: | 1356992-21-6 | MF: | C21H22ClF2N3O8S | MW: | 549.93 | EINECS: | | Product Categories: | | Mol File: | 1356992-21-6.mol | ![XL-784 free base Structure](CAS/20210111/GIF/1356992-21-6.gif) |
| XL-784 free base Chemical Properties |
density | 1.507±0.06 g/cm3(Predicted) | storage temp. | Store at -20°C | solubility | DMSO: 250 mg/mL (454.60 mM) | pka | 9.38±0.23(Predicted) |
| XL-784 free base Usage And Synthesis |
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 |
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