CAS NO: | 668270-12-0 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
100mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
10 g | 电议 |
生物活性 | Linagliptin is a highly potent, selectiveDPP-4inhibitor withIC50of 1 nM. | ||||||||||||||||
IC50& Target | IC50: 1 nM (DPP-4) | ||||||||||||||||
体外研究 (In Vitro) | Linagliptin inhibits DPP-4 activity in vitro in several independent experiments with IC50values of 0.4, 0.5, 0.9, and 1.1 nM (mean IC50, approximately 1 nM). Linagliptin inhibits FAP with an IC50of 89 nM (approximately 90-fold selectivity versus DPP-4)[2]. | ||||||||||||||||
体内研究 (In Vivo) | In male Wistar rats, Beagle dogs, and Rhesus monkeys, xanthine linagliptin proves to be a highly efficacious, long-lasting, and potent DPP-4 inhibitor providing >70% inhibition for >7 h for all three species after oral administration of 1 mg/kg. Single oral administration of linagliptin to db/db mice 45 min prior to an oral glucose tolerance test reduced plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition)[1]. Linagliptin (3 and 10 mg/kg) dose-dependently inhibits the DPP-4 enzyme in plasma within 30 min of administration. Linagliptin (1 mg/kg, p.o.) significantly reduces glucose excursion by approximately 50%[2]. Oral administration of the DPP-4 inhibitor linagliptin (3 mg/kg, p.o.) strongly reduces DPP-4 activity, stabilizes active GLP-1 in chronic wounds, and improves healing in ob/ob mice. At day 10 postwounding, linagliptin-treated ob/ob mice show largely epithelialized wounds characterized by the absence of neutrophils[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 472.54 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C25H28N8O2 | ||||||||||||||||
CAS 号 | 668270-12-0 | ||||||||||||||||
中文名称 | 利格列汀;利拉利汀;利格利汀 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(52.91 mM;ultrasonic and warming and heat to 80℃) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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