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 。
货号:ajcx35776
CAS:217178-62-6
分子式:C20H23BrN3O8P
分子量：544.29
溶解度:DMSO : 100 mg/mL (183.73 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively[1].

Stampidine (7.8-1,000 μM; 24 hours) is not cytotoxic to genital tract epithelial cells[2].Stampidine has no effect on sperm motility in cervical mucus[2].

Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats[3].Stampidine (100 mg/kg; p.o.) shows the average plasma Cmax, AUC, half-life (t1/2), and mean residence time (MRT) values of 15.4 µM, 23.1 µM•h, 108.6 min and 119.4 min, respectively, in dogs[4].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[4].

[1]. Osmond J D’Cruz, et al. Stampidine: a selective oculo-genital microbicide. J Antimicrob Chemother. 2005 Jul;56(1):10-9.
[2]. Osmond J D’Cruz, et al. Stampidine is a potential nonspermicidal broad-spectrum anti-human immunodeficiency virus microbicide. Fertil Steril. 2004 Mar;81 Suppl 1:831-41.
[3]. Fatih M Uckun, et al. In Vivo Antiretroviral Activity of Stampidine in Chronically Feline Immunodeficiency Virus-Infected Cats. Antimicrob Agents Chemother. 2003 Apr;47(4):1233-40.
[4]. Fatih M Uckun, et al. In Vivo Pharmacokinetics and Toxicity Profile of the anti-HIV Agent Stampidine in Dogs and Feline Immunodeficiency Virus-Infected Cats. Arzneimittelforschung. 2006 Feb;56(2A):176-92.