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GS7340
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
GS7340图片
CAS NO:379270-37-8
包装与价格：
包装价格(元)
5mg询价
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Oral prodrug of Tenofovir
Cas No.379270-37-8
别名替诺福韦艾拉酚胺; GS-7340
化学名(2S)-isopropyl 2-((((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate
Canonical SMILESCC(OC([C@](NP(COC(CN1C=NC(C1=NC=N2)=C2N)([H])C)(OC3=CC=CC=C3)=O)([H])C)=O)C.O=C(O)/C([H])=C([H])/C(O)=O
分子式C21H29N6O5P
分子量476.47
溶解度DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 15 mg/ml,PBS (pH 7.2): 2 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[1].  Callebaut C, Stepan G, Tian Y, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother, 2015, 59(10): 5909-5916.
[2].  Margot NA, Johnson A, Miller MD, et al. Characterization of HIV-1 Resistance to Tenofovir Alafenamide In Vitro. Antimicrob Agents Chemother, 2015, 59(10): 5917-5924.
[3].  Murakami E, Wang T, Park Y, et al. Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy. Antimicrob Agents Chemother, 2015, 59(6): 3563-3569.

 
 
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