| CAS NO: | 379270-37-8 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 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 SMILES | CC(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 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 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: |
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