購物車 
-
替諾福韋阿拉芬酰胺富馬酸酯
- names：
Tenofovir alafenamide fumarate
- CAS號：
379270-38-9
MDL Number： - MF(分子式)： C25H33N6O9P MW(分子量)： 592.54
- EINECS: Reaxys Number:
- Pubchem ID:68516365 Brand:BIOFOUNT
替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]也稱為替諾福韋阿拉芬酰胺半富馬酸鹽；TAF GS-7340是核苷酸逆轉錄酶抑制劑和替諾福韋的新型前藥。吉利德科學公司正在開發它，用于治療HIV感染。與常用的逆轉錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關，與該藥劑相比，替諾福韋阿拉芬酰胺具有更大的抗病毒活性和更好的向淋巴組織的分布。吉利德（Gilead）宣布了一項三階段臨床試驗，該試驗評估了將GS-7340與考比司他，恩曲他濱和elvitegravir組合使用的單片方案，并計劃與cobicistat，恩曲他濱和蛋白酶抑制劑darunavir共同配制該藥物。
| 貨品編碼 | 規格 | 純度 | 價格 (￥) | 現價(￥) | 特價(￥) | 庫存描述 | 數量 | 總計 (￥) |
|---|---|---|---|---|---|---|---|---|
| YZM000631-10mg | 10mg | 99.78% | ￥ 911.00 | ￥ 911.00 | 2-3天 | ￥ 0.00 | ||
| YZM000631-5mg | 5mg | 99.78% | ￥ 585.00 | ￥ 585.00 | 2-3天 | ￥ 0.00 |
| 中文別名 | 替諾福韋阿拉芬酰胺富馬酸酯(379270-38-9);替諾福韋艾拉酚胺富馬酸鹽;替諾福韋阿拉芬酰胺富馬酸鹽;替諾福韋阿拉芬酰胺半富馬酸鹽; GS-7340富馬酸酯; GS 7340富馬酸酯; GS7340富馬酸酯; （S）-異丙基2-（（（（S）-（（（（R）-1-（6-amino-9H-purin-9-yl）prop-2--2-yl）oxy）甲基）（苯氧基）磷酰基）氨基）丙酸酯富馬酸酯; TAF；GS734; GS-734；GS 7340；替諾福韋阿拉芬酰胺富馬酸酯; 商品名稱：Genvoya; |
| 英文別名 | Tenofovir alafenamide fumarate(379270-38-9);GS-7340 (fumarate); GS-7340 fumarate; GS 7340 fumarate; GS7340 fumarate; (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate fumarate; TAF; GS734; GS-734; GS 7340; Tenofovir alafenamide fumarate; trade name; |
| CAS號 | 379270-38-9 |
| Inchi | InChI=1S/C21H29N6O5P.C4H4O4/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27;5-3(6)1-2-4(7)8/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24);1-2H,(H,5,6)(H,7,8)/b;2-1+/t15-,16+,33-;/m1./s1 |
| InchiKey | MEJAFWXKUKMUIR-BVSQZBJNSA-N |
| 分子式 Formula | C25H33N6O9P |
| 分子量 Molecular Weight | 592.54 |
| 溶解度Solubility | 生物體外In Vitro:DMSO溶解度≥ 36 mg/mL(60.76 mM)H2O≥ 25 mg/mL(42.19 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知. |
| 性狀 | 白色至類白色固體粉末,Power |
| 儲藏條件 Storage conditions | -20°C 3 years年 4°C 2 years年 / In solvent溶液中:-80°C 6 months月 -20°C 1 month月 |
替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質及有害物質產生，必要時實驗操作需要手套箱內完成以免對實驗人員造成傷害
3.實驗后產生的廢棄物需分類存儲，并交于專業生物廢氣物處理公司處理，以免造成環境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.
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| 產品說明 | 替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]是 Tenofovir 的前體,Tenofovir是一種有效的HIV-1核苷酸逆轉錄酶的抑制劑 |
| Introduction | 替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]is an investigational oral prodrug of Tenof ovir. Tenof ovir is aHIVnucleotide reverse transcriptase inhibitor. |
| Application1 | Tenofovir alafenamide fumarate (GS-7340 fumarate) 是 Tenofovir 的前體，Tenofovir 是一種 HIV-1 核苷酸逆轉錄酶抑制劑。 |
| Application2 | |
| Application3 |
替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]藥理學：
1、替諾福韋阿拉芬酰胺富馬酸酯，也稱為替諾福韋阿拉芬酰胺半富馬酸鹽；TAF GS-7340是核苷酸逆轉錄酶抑制劑和替諾福韋的新型前藥。吉利德科學公司正在開發它，用于治療HIV感染。與常用的逆轉錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關，與該藥劑相比，替諾福韋阿拉芬酰胺具有更大的抗病毒活性和更好的向淋巴組織的分布。吉利德（Gilead）宣布了一項三階段臨床試驗，該試驗評估了將GS-7340與考比司他，恩曲他濱和elvitegravir組合使用的單片方案，并計劃與cobicistat，恩曲他濱和蛋白酶抑制劑darunavir共同配制該藥物。
2、替諾福韋阿拉法酰胺富馬酸酯（GS-7340富馬酸酯）是替諾福韋的前體，替諾福韋是一種HIV-1核苷酸逆轉錄酶抑制劑。
1、替諾福韋阿拉芬酰胺富馬酸酯，也稱為替諾福韋阿拉芬酰胺半富馬酸鹽；TAF GS-7340是核苷酸逆轉錄酶抑制劑和替諾福韋的新型前藥。吉利德科學公司正在開發它，用于治療HIV感染。與常用的逆轉錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關，與該藥劑相比，替諾福韋阿拉芬酰胺具有更大的抗病毒活性和更好的向淋巴組織的分布。吉利德（Gilead）宣布了一項三階段臨床試驗，該試驗評估了將GS-7340與考比司他，恩曲他濱和elvitegravir組合使用的單片方案，并計劃與cobicistat，恩曲他濱和蛋白酶抑制劑darunavir共同配制該藥物。
2、替諾福韋阿拉法酰胺富馬酸酯（GS-7340富馬酸酯）是替諾福韋的前體，替諾福韋是一種HIV-1核苷酸逆轉錄酶抑制劑。
| 警示圖 | |
| 危險性 | warning |
| 危險性警示 | Not available |
| 安全聲明 | H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害 |
| 安全防護 | P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續沖洗+P337如果眼睛刺激持續+P2393獲得醫療建議/護理 |
| 備注 | 實驗過程中防止吸入、食入，做好安全防護 |
替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]危害標識：
| 象形圖 |  |
| 信號 | Warning |
| GHS危險說明 | The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory. |
| H373 (100%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure] | |
| 防范說明代碼 | P260, P314, and P501 |
| (The corresponding statement to each P-code can be found at the GHS Classification page.) |
| Babusis D, et al. Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340. Mol Pharm. 2013 Feb 4;10(2):459-66. |
| Ruane PJ, et al. Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults. J Acquir Immune Defic Syndr. 2013 Aug 1;63(4 |
替諾福韋阿拉芬酰胺富馬酸酯[379270-38-9,Tenofovir alafenamide fumarate,GS-7340 (fumarate)]參考文獻：
1.Adenine: an important drug scaffold for the design of antiviral agents.
Wang C;Song Z;Yu H;Liu K;Ma X Acta Pharm Sin B. 2015 Sep;5(5):431-41. doi: 10.1016/j.apsb.2015.07.002. Epub 2015 Sep 2.
Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well-known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modifications on the scaffold itself and the peripheral sections were made. The structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.
2、Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults
Peter J Ruane 1, Edwin DeJesus, Daniel Berger, Martin Markowitz, U Fritz Bredeek, Christian Callebaut, Lijie Zhong, Srini Ramanathan, Martin S Rhee, Marshall W Fordyce, Kitty Yale
Abstract Objective: To evaluate the antiviral activity, safety, pharmacokinetics, and pharmacokinetics/pharmacodynamics of short-term monotherapy with tenofovir alafenamide (TAF), a next-generation tenofovir (TFV) prodrug. Design: A phase 1b, randomized, partially blinded, active- and placebo-controlled, dose-ranging study. Methods: Treatment-naive and experienced HIV-1-positive adults currently off antiretroviral therapy were randomized to receive 8, 25, or 40 mg TAF, 300 mg tenofovir disoproxil fumarate (TDF), or placebo, each once daily for 10 days. Results: Thirty-eight subjects were enrolled. Baseline characteristics were similar across dose groups. Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg. At steady state, 8, 25, and 40 mg TAF yielded mean TFV plasma exposures [area under the plasma concentration-time curve (AUCtau)] of 97%, 86%, and 79% lower, respectively, as compared with the TFV exposures observed with 300 mg TDF. For 25 and 40 mg TAF, the mean intracellular peripheral blood mononuclear cell tenofovir diphosphate AUCtau was ∼7-fold and ∼25-fold higher, relative to 300 mg TDF. Conclusions: Compared with 300 mg TDF, TAF demonstrated more potent antiviral activity, higher peripheral blood mononuclear cell intracellular tenofovir diphosphate levels, and lower plasma TFV exposures, at approximately 1/10th of the dose. This may translate into greater antiviral efficacy, a higher barrier to resistance, and an improved safety profile relative to TDF, supporting further investigation of TAF dosed once daily in HIV-infected patients.
1.Adenine: an important drug scaffold for the design of antiviral agents.
Wang C;Song Z;Yu H;Liu K;Ma X Acta Pharm Sin B. 2015 Sep;5(5):431-41. doi: 10.1016/j.apsb.2015.07.002. Epub 2015 Sep 2.
Adenine derivatives, in particular the scaffold bearing the acyclic nucleoside phosphonates (ANPS), possess significant antiviral and cytostatic activity. Till now, several effective adenine derivatives have been marketed for the treatment of HIV, HBV, CMV and other virus-infected diseases. These compounds are represented by tenofovir (PMPA), a medicine for both HIV and HBV, and adefovir as an anti-HBV agent. More than this, other analogs, such as GS9148, GS9131, and GS7340, are also well-known anti-viral agents that have been progressed to the clinical studies for their excellent activity. In general, the structures of these compounds include an adenine nucleobase linked to a phosphonate side chain. Considerable structural modifications on the scaffold itself and the peripheral sections were made. The structure-activity relationships (SARs) of this skeleton will provide valuable clues to identify more effective adenine derivatives as antiviral drugs. Here, we systematically summarized the SARs of the adenine derivatives, and gave important information for further optimizing this template.
2、Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults
Peter J Ruane 1, Edwin DeJesus, Daniel Berger, Martin Markowitz, U Fritz Bredeek, Christian Callebaut, Lijie Zhong, Srini Ramanathan, Martin S Rhee, Marshall W Fordyce, Kitty Yale
Abstract Objective: To evaluate the antiviral activity, safety, pharmacokinetics, and pharmacokinetics/pharmacodynamics of short-term monotherapy with tenofovir alafenamide (TAF), a next-generation tenofovir (TFV) prodrug. Design: A phase 1b, randomized, partially blinded, active- and placebo-controlled, dose-ranging study. Methods: Treatment-naive and experienced HIV-1-positive adults currently off antiretroviral therapy were randomized to receive 8, 25, or 40 mg TAF, 300 mg tenofovir disoproxil fumarate (TDF), or placebo, each once daily for 10 days. Results: Thirty-eight subjects were enrolled. Baseline characteristics were similar across dose groups. Significant reductions in plasma HIV-1 RNA from baseline to day 11 were observed for all TAF dose groups compared with placebo (P < 0.01), with a median decrease of 1.08-1.73 log10 copies per milliliter, including a dose-response relationship for viral load decrease up to 25 mg. At steady state, 8, 25, and 40 mg TAF yielded mean TFV plasma exposures [area under the plasma concentration-time curve (AUCtau)] of 97%, 86%, and 79% lower, respectively, as compared with the TFV exposures observed with 300 mg TDF. For 25 and 40 mg TAF, the mean intracellular peripheral blood mononuclear cell tenofovir diphosphate AUCtau was ∼7-fold and ∼25-fold higher, relative to 300 mg TDF. Conclusions: Compared with 300 mg TDF, TAF demonstrated more potent antiviral activity, higher peripheral blood mononuclear cell intracellular tenofovir diphosphate levels, and lower plasma TFV exposures, at approximately 1/10th of the dose. This may translate into greater antiviral efficacy, a higher barrier to resistance, and an improved safety profile relative to TDF, supporting further investigation of TAF dosed once daily in HIV-infected patients.
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