Tenofovir Disoproxil Fumarate

別名: GS 1278, Tenofovir DF 中文名稱：富馬酸替諾福韋酯

目錄號：S1400 Purity: 99.94%

Tenofovir Disoproxil Fumarate屬于一類抗逆轉(zhuǎn)錄病毒藥物，其通過與天然底物脫氧腺苷5’-三磷酸鹽競爭以及整合到DNA后終止DNA鏈抑制HIV reverse transcriptase活性。

Tenofovir Disoproxil Fumarate Chemical Structure

CAS: 202138-50-9

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1056.27	現(xiàn)貨
10mg	809.18	現(xiàn)貨
50mg	2554.21	現(xiàn)貨
1g	10401.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.94%

99.94

Tenofovir Disoproxil Fumarate相關(guān)產(chǎn)品

相關(guān)靶點	HBV RT HIV RT RT	點擊展開
相關(guān)產(chǎn)品	Dapivirine (TMC120) Salicylanilide Fangchinoline	點擊展開
相關(guān)化合物庫	抗感染化合物庫抗生素化合物庫抗病毒化合物庫抗寄生蟲藥物庫腸道微生物代謝物庫	點擊展開

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系	實驗類型	孵育時間	活性描述	文獻信息
HepG2	Antiviral assay	9 days	Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=5.1μM	17888662
HepG2	Cytotoxicity assay	9 days	Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=2.31μM	17888662
MT2	Function assay	5 days	Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days, EC50=0.015μM	17562366
human bone marrow cells	Cytotoxicity assay	24 hrs	Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9μM	20439609
human bone marrow cells	Cytotoxicity assay	24 hrs	Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay, CC50=1.9μM	20439609
HeLa-T4	Antiviral assay	48 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50=0.0029μM	21060108
HeLa-T4	Antiviral assay	48 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95=0.037μM	21060108
HeLaT4	Antiviral assay	24 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50=0.12μM	21060108
HeLaT4	Function assay	24 hrs	Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs	21060108
HeLaT4	Antiviral assay	24 hrs	Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed	21060108
PBMC	Antiviral assay	7 days	Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive inc, EC50=0.0046μM	27405794
HepG2.2.15	Antiviral assay	3 days	Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA in cell supernatant incubated for 3 days in presence of 10% FBS followed by compound treatment in absence of 10% FBS for 3 days by qRT-PCR method, EC50=0.34μM	27405794
HepG2.2.15	Cytotoxicity assay	6 days	Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay, CC50=29.2μM	27405794
PBMC	Antiviral assay	30 mins	Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured, IC50=0.08μM	28682067
PBMC	Antiviral assay	30 mins	Antiviral activity against CCR5 tropic HIV1 BaL infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on , IC50=0.22μM	28682067
MT4	Antiviral assay	6 days	Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay, EC50=4.89μM	28682067
MT4	Antiviral assay	6 days	Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d, EC50=11.3μM	28682067
MT2	Antiviral assay		Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.54μM	19596885
MT-2	Antiviral assay		Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50=0.0068μM	19104010
HeLa P4/R5	Antiviral assay		Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7μM	19596885
HeLa P4/R5	Antiviral assay		Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4μM	19596885
HeLaT4	Antiviral assay		Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC99.6=0.95μM	21060108
HeLaT4	Cytotoxicity assay		Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34μM	21060108
HepG2.2.15	Antiviral assay		Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=0.85μM	31223460
HepG2.2.15	Cytotoxicity assay		Cytotoxicity against human HepG2.2.15 cells infected with HBV, CC50=20.71μM	31223460
點擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

HIV reverse transcriptase ^[1]
(Cell-free assay)

體外研究(In Vitro)
體外研究活性	Tenofovir的循環(huán)經(jīng)腎臟通過腎小球濾過和腎小管主動分泌。Tenofovir不是人有機陽離子轉(zhuǎn)運1型（hOCT1）或hOCT2的底物。在MRP4過表達細(xì)胞中，Tenofovir積累到五倍較低水平，MRP抑制劑可提高其累積。^[1] 在人肝母細(xì)胞瘤（肝癌）細(xì)胞，骨骼肌細(xì)胞（SkMCs）或腎近端小管上皮細(xì)胞中，Tenofovir并不顯著影響線粒體DNA（mtDNA）的。在HepG2細(xì)胞或SkMCs中，Tenofovir升高的乳酸生產(chǎn)小于20％。^[2] 在HepG2細(xì)胞和人原代肝細(xì)胞中，Tenofovir是替諾福韋二磷酸（TFV-DP）有效的磷酸化。在基于細(xì)胞的測定中，Tenofovir抗HBV的50％有效濃度是1.1 mM，加入bis-isoproxil前基團之后有效率提高50倍。在體外和臨床中，Tenofovir對lamivudine耐藥HBV有充分的活動。^[3] Tenofovir抑制肝源性肝癌細(xì)胞和正常骨骼肌細(xì)胞的增殖，CC（50）值分別為398 μM和870 μM。Tenofovir比cidofovir對腎近曲小管上皮細(xì)胞的增殖和生存能力影響弱，cidofovir具有潛在的相關(guān)的核苷酸類似物誘導(dǎo)腎小管功能障礙。^[4]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05874440	Recruiting	Chronic Hepatitis b Patients	Sohag University	April 15 2023	--
NCT03576066	Completed	Chronic Hepatitis B	Assembly Biosciences	June 11 2018	Phase 2
NCT03361956	Completed	Hepatitis B	Janssen Sciences Ireland UC	February 13 2018	Phase 2
NCT02985996	Completed	HIV Infections	Emory University\|Centers for Disease Control and Prevention	February 6 2017	Phase 1

參考文獻
[1] Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304. [2] Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723. [3] Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477. [4] Cihlar T, et al. Antiviral Res, 2002, 54(1), 37-45. [5] Taneva E, et al. Antimicrob Agents Chemother. 2015, 60(3):1667-75. [6] Ng HH, et al. Int J Toxicol. 2015, 34(1):4-10. + 展開

參考文獻

[1] Ray AS, et al. Antimicrob Agents Chemother, 2006, 50(10), 3297-3304.
[2] Birkus G, et al. Antimicrob Agents Chemother, 2002, 46(3), 716-723.
[3] Delaney WE 4th, et al. Antimicrob Agents Chemother, 2006, 50(7), 2471-2477.

[4] Cihlar T, et al. Antiviral Res, 2002, 54(1), 37-45.
[5] Taneva E, et al. Antimicrob Agents Chemother. 2015, 60(3):1667-75.
[6] Ng HH, et al. Int J Toxicol. 2015, 34(1):4-10.

+ 展開

化學(xué)信息&溶解度

分子量	635.51	分子式	C₁₉H₃₀N₅O₁₀P.C₄H₄O₄
CAS號	202138-50-9	SDF	Download Tenofovir Disoproxil Fumarate SDF
Smiles	CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (157.35 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 100 mg/mL (157.35 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (157.35 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 4 mg/mL (6.29 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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