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217178-62-6

中文名称 Stampidine
英文名称 Stampidine
CAS 217178-62-6
分子式 C20H23BrN3O8P
分子量 544.29
MOL 文件 217178-62-6.mol
217178-62-6 结构式 217178-62-6 结构式

基本信息

中文别名
化合物 T24839
英文别名
HI 113
Sampidine
Stampidine

物理化学性质

储存条件-20°C储存
溶解度DMSO : 100 mg/mL (183.73 mM; Need ultrasonic)
形态Solid
颜色White to off-white

常见问题列表

生物活性
Stampidine 是一种核苷逆转录酶抑制剂 (NRTI),具有高效、广谱的抗 HIV 活性。Stampidine 抑制实验室 HIV-1 株 HTLVIIIB (B 包膜亚型) 和主要临床分离株的 IC50 值分别为 1 nM 和 2 nM。Stampidine 还可以抑制耐 NRTI 临床分离株和耐 NNRTI 临床分离株,IC50 分别为 8.7 nM 和 11.2 nM 。
靶点

IC50: 1 nM (HTLV IIIB ), 2 nM (primary clinical isolates), 8.7 nM (NRTI-resistant primary clinical isolates), 11.2 nM (NRTI-resistant primary clinical isolates)

体外研究

Stampidine (7.8-1,000 μM; 24 hours) is not cytotoxic to genital tract epithelial cells.
Stampidine has no effect on sperm motility in cervical mucus.

体内研究

Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats.
Stampidine (100 mg/kg; p.o.) shows the average plasma C max , AUC, half-life (t 1/2 ), and mean residence time (MRT) values of 15.4 µM, 23.1 µM•h, 108.6 min and 119.4 min, respectively, in dogs.
Stampidine does not cause anemia, thrombocytopenia, neutropenia, or lymphopenia suggestive of hematologic toxicity, elevations of BUN or creatinine or electrolyte disturbances suggestive of renal toxicity or metabolic abnormalities, elevations of ALT, AST, Alk in adult beagle dogs.

Animal Model: SPF male or female domestic cats (2.9- 6.2 kg), with chronically FIV-infected
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral administration (oral bolus dose)
Result: Exhibited potent antiretroviral activity.
Animal Model: Male beagle dogs (10-12 kg)
Dosage: 100 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: The estimated average plasma C max and AUC values were 15.4 µM and 23.1 µM·h, respectively. The average elimination half-life (t 1/2 ) and mean residence time (MRT) were 108.6 min and 119.4 min, respectively.
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