α-Glucosidase-IN-16 是一种有效且具有口服活性的 α-葡萄糖苷酶 (α-Glucosidase) 抑制剂,IC50为 3.28 μM。α-Glucosidase-IN-16 可降低链脲佐菌素 (Streptozotocin) 诱导的糖尿病大鼠的血糖水平。具有抗糖尿病活性。
产品描述
α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC 50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin -induced diabetic rats. Antidiabetic activity [1].
体内活性
α-Glucosidase-IN-16 (compound 13B) (10 and 20 mg/kg; PO; once daily for 28 days) significantly reduces the level of blood glucose in diabetic rats [1]. α-Glucosidase-IN-16 (2000 mg/kg; PO; single dosage) exhibits no toxic effects in mice [1]. α-Glucosidase-IN-16 (10 and 20 mg/kg; PO; single dosage) significantly reduces serum glucose level after glucose administration in rats [1]. Animal Model: Wistar rats (170-200 g, 8-10 weeks; induced diabetes by intraperitoneal injection of Streptozotocin ) [1] Dosage: 10 and 20 mg/kg Administration: PO; once daily for 28 days Result: Caused a significant reduction in the level of blood glucose compared to diabetic control. Lowered the total cholesterol level. Effect of α-Glucosidase-IN-16 on blood glucose (mg/dL) in Streptozotocin -induced diabetes [1]. dose (mg/kg) day 1 day 7 day 14 day 21 day 28 10 370.81 ± 4.79 289.89 ± 4.33 200.33 ± 4.57 149.30 ± 4.56 132.98 ± 4.33 20 375.31 ± 5.01 230.71 ± 4.88 163.68 ± 4.37 120.72 ± 4.11 108.42 ± 3.98 Animal Model: Balb/C mice [1] Dosage: 2000 mg/kg Administration: PO; single dosage (acute toxicity study) Result: Exhibited no toxic effects (via observing signs of diarrhea, convulsions, lethargy, sleeping, salivation, and tremor). Animal Model: Wistar rats (oral administration with 3 g/kg glucose) [1] Dosage: 10 and 20 mg/kg Administration: PO; single dosage (oral glucose tolerance test) Result: Significantly reduced serum glucose level (110-113 mg/dL) compared to the control group (128 mg/dL) after 2 hours of glucose administration.
Cas No.
1606142-34-0
分子式
C22H18FNS
分子量
347.45
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years