購(gòu)物車 
-
替諾福韋阿拉芬酰胺富馬酸酯
- names：
Tenofovir alafenamide fumarate
- CAS號(hào)：
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(zhuǎn)錄酶抑制劑和替諾福韋的新型前藥。吉利德科學(xué)公司正在開(kāi)發(fā)它，用于治療HIV感染。與常用的逆轉(zhuǎn)錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關(guān)，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(xiàng)三階段臨床試驗(yàn)，該試驗(yàn)評(píng)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(jì)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(guī)格 | 純度 | 價(jià)格 (￥) | 現(xiàn)價(jià)(￥) | 特價(jià)(￥) | 庫(kù)存描述 | 數(shù)量 | 總計(jì) (￥) |
|---|---|---|---|---|---|---|---|---|
| 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 |
- 大包裝詢價(jià) 提供各種包裝，敬請(qǐng)垂詢
- 收藏商品 商品點(diǎn)評(píng) 加入購(gòu)物車 立即購(gòu)買
| 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?；┌被┍狨ジ获R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(hào) | 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(chǔ)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(shí)驗(yàn)注意事項(xiàng)：
1.實(shí)驗(yàn)前需戴好防護(hù)眼鏡，穿戴防護(hù)服和口罩，佩戴手套，避免與皮膚接觸。
2.實(shí)驗(yàn)過(guò)程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時(shí)實(shí)驗(yàn)操作需要手套箱內(nèi)完成以免對(duì)實(shí)驗(yàn)人員造成傷害
3.實(shí)驗(yàn)后產(chǎn)生的廢棄物需分類存儲(chǔ)，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)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.
Tags:GS-7340 (fumarate)試劑,GS-7340 (fumarate)雜質(zhì),GS-7340 (fumarate)中間體,GS-7340 (fumarate)合成,GS-7340 (fumarate)密度,GS-7340 (fumarate)溶解度,GS-7340 (fumarate)旋光度,GS-7340 (fumarate)閃點(diǎn),GS-7340 (fumarate)購(gòu)買,
| 產(chǎn)品說(shuō)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(zhuǎn)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(zhuǎn)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(xué)：
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(zhuǎn)錄酶抑制劑和替諾福韋的新型前藥。吉利德科學(xué)公司正在開(kāi)發(fā)它，用于治療HIV感染。與常用的逆轉(zhuǎn)錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關(guān)，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(xiàng)三階段臨床試驗(yàn)，該試驗(yàn)評(píng)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(jì)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(zhuǎn)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(zhuǎn)錄酶抑制劑和替諾福韋的新型前藥。吉利德科學(xué)公司正在開(kāi)發(fā)它，用于治療HIV感染。與常用的逆轉(zhuǎn)錄酶抑制劑富馬酸替諾福韋二甲氧吡啶（Viread）密切相關(guān)，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(xiàng)三階段臨床試驗(yàn)，該試驗(yàn)評(píng)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(jì)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(zhuǎn)錄酶抑制劑。
| 警示圖 | |
| 危險(xiǎn)性 | warning |
| 危險(xiǎn)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(duì)身體有害 |
| 安全防護(hù) | P264處理后徹底清洗+P280戴防護(hù)手套/穿防護(hù)服/戴防護(hù)眼罩/戴防護(hù)面具+P305如果進(jìn)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(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護(hù)理 |
| 備注 | 實(shí)驗(yàn)過(guò)程中防止吸入、食入，做好安全防護(hù) |
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(biāo)識(shí)：
| 象形圖 |  |
| 信號(hào) | Warning |
| GHS危險(xiǎn)說(shuō)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(shuō)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(xiàn)：
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.
對(duì)不起，暫無(wú)產(chǎn)品評(píng)價(jià)！
MSDS
SDS 1.0 中文
展開(kāi)
SDS 1.0 英文
展開(kāi)
- 相關(guān)產(chǎn)品
-
< >
- 推薦產(chǎn)品
-
< >
- 最新產(chǎn)品
-
< >
新聞
胞爬片免疫組化染色.png)
怎么做細(xì)胞爬片免疫組化染色實(shí)驗(yàn)
細(xì)胞爬片免疫組化染色，是通過(guò)細(xì)胞爬片是讓玻片浸在細(xì)胞培養(yǎng)基內(nèi)，細(xì)胞在玻片上生長(zhǎng)，主要用于組織學(xué)，免疫組織化學(xué)...
2020/7/20 22:04:33
提取病毒RNA的實(shí)驗(yàn)方法
提取病毒RNA方法分別有：異硫氰酸胍的提取病毒RNA方法、TRIzol LS提取法、Trizol法提取法等等...
2020/7/22 20:29:26
脂.png)
chelex 100樹(shù)脂國(guó)產(chǎn)替代之路-BIOFOUNT范德生物
Chelex 100螯合離子交換樹(shù)脂對(duì)銅、鐵和其他重金屬?的偏好顯著高于對(duì)鈉、鉀等一價(jià)陽(yáng)離子的偏好。它對(duì)二價(jià)...
2025/11/4 14:22:46
9月開(kāi)學(xué)季——助研新學(xué)期 范德送好禮
2025/8/28 15:30:55
Waxfilm 實(shí)驗(yàn)室封口膜：技術(shù)與國(guó)際市場(chǎng)的雙重突破
在實(shí)驗(yàn)室耗材領(lǐng)域，封口膜是保障實(shí)驗(yàn)準(zhǔn)確性與穩(wěn)定性的關(guān)鍵產(chǎn)品之一。近年來(lái)，Waxfilm?實(shí)驗(yàn)室封口膜憑借其卓...
2025/5/13 13:03:40
Waxfilm實(shí)驗(yàn)室封口膜的5大突破
Waxfilm實(shí)驗(yàn)室封口膜作為生物功能膜領(lǐng)域的國(guó)產(chǎn)技術(shù)突破和品牌突破，是生物領(lǐng)域中國(guó)技術(shù)發(fā)展的縮影。
2025/5/6 17:02:07
各種微流控芯片鍵合方法的優(yōu)缺點(diǎn)
微流控芯片鍵合：目前主要有激光焊接、熱壓鍵合、膠鍵合、超音波焊接，每種方法都有各自的優(yōu)缺點(diǎn)。本文主要介紹聚酯...
2023/7/28 10:43:09
新一代微流控鍵合解決方案
微流控鍵合解決方案：微流控芯片制造的一個(gè)重要環(huán)節(jié)，也是最容易被忽視的--芯片鍵合。其中一個(gè)重要因素是：微流控...
2023/7/27 12:44:28
驗(yàn)動(dòng)物圖.png)
熒光素鉀鹽使用說(shuō)明
D-熒光素鉀鹽（K+）設(shè)計(jì)用于體外和體內(nèi)生物發(fā)光測(cè)定。D-熒光素的質(zhì)量和純度對(duì)于獲得良好和可重復(fù)的結(jié)果至關(guān)重...
2023/7/20 11:05:11
如何選BSA（牛血清白蛋白）
如何選BSA（牛血清白蛋白）：牛血清白蛋白（BSA）有多種形式，如何選擇適合自己的牛血清白蛋白（BSA）是一...
2023/2/14 13:09:18
