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化學性質:
規格 | 5mg 10mg 50mg 100mg |
CAS | 379270-38-9/379270-37-8 |
別名 |
|
化學名 | (2S)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate |
分子式 | C25H33N6O9P |
分子量 | 592.54 |
溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 15 mg/ml,PBS (pH 7.2): 2 mg/ml |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
GS7340 (Tenofovir Alafenamide, TAF) is a novel oral prodrug of Tenofovir with improved antiviral activity [1].
Tenofovir (TFV) is an HIV-1 nucleotide reverse transcriptase (RT) inhibitor for the treatment of HIV infections [1].
GS7340 (Tenofovir Alafenamide, TAF) is a novel oral prodrug of Tenofovir. In peripheral blood mononuclear cells, TAF is mostly converted to TFV and achieved higher tenofovir diphosphate (TFV-DP) levels, compared with TDF. In MT-2 and MT-4 cells infected with HIV-1IIIB, TAF exhibited anti-HIV-1 activity with EC50 values of 5 nM, while with CC50 (50% cell death) values of 42 and 4.7 nM, respectively. In the 29 primary HIV-1 isolates tested in PBMCs, EC50 values of TAF ranged from 0.10 to 12.0 nM with mean EC50 of 3.5 nM. For the HIV-2 isolates, the mean EC50 value was 1.8 nM. In MT-2 cells, TAF maintained its antiviral activity after HS (human serum) pretreatment, suggesting its plasma stability. TAF is a potent inhibitor of immunodeficiency viruses, such as HIV and SIV, and a weak inhibitor of HSV-2 [1]. In HIV-1 isolates with NRTI resistance amino acid substitutions, TAF exhibited reduced activity [2]. In primary human hepatocytes, TAF resulted in high levels of tenofovir diphosphate (TFV-DP), which exhibited half-life of >24 h [3].
In dogs, TAF orally administration for 7 days increased the levels of TFV-DP in dog livers for the treatment of HBV infection [3].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278