产品
编 号:F750617
分子式:C16H18ClNO3S2
分子量:371.9
产品类型
结构图
CAS No: 2252493-33-5
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产品详情
生物活性:
(R)-ND-336 is a potent and selective MMP-9 inhibitor with a Ki of 19 nM. (R)-ND-336 inhibits MMP-2 (Ki=127 nM) and MMP-14 (Ki=119 nM). (R)-ND-336 has the potential for diabetic foot ulcers (DFUs) research.
体内研究:
(R)-ND-336 (50 μg/wound/day for 14 days) accelerates wound healing faster. (R)-ND-336 has an AUC of 1.3 μM?min after topical administration and 35 μM?min following intravenous dosing, for an AUCtop/AUCiv ratio of 3.7%, indicating minimal absorption after topical administration in db/db mice. Animal Model:Female db/db mice (BKS.Cg-Dock7m+/+Leprdb/J, 8-weeks old, ~40 g body weight)
Dosage:50 μg
Administration:Wound; once a day for 14 days
Result:Accelerated wound healing faster and showed complete inhibition of MMP-9.
体外研究:
(R)-ND-336 poorly inhibits other MMPs (Ki>100 μM). (R)-ND-336 has a long residence time (the time the inhibitor is bound to MMP-9, calculated as 1/koff) of 300 min. A favorable IC50value of 143 μM afforded a therapeutic index (IC50/Ki for MMP-9) ratio of 7530, indicating that (R)-ND-336 is not cytotoxic.