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替诺福韦

逆转录酶抑制剂

规格或纯度: ≥99%

CAS编号: 147127-20-6
分子式: C₉H₁₄N₅O₄P
分子量: 287.22
MDL号: MFCD00943794
PubChem编号: 464205

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货号 (SKU)	包装规格	是否现货	价格	数量
T125736-1g	1g	现货
T125736-5g	5g	现货
T125736-25g	25g	现货
T125736-100g	100g	现货
T125736-500g	500g	现货

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六元杂环化合物膦酸类

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基本描述

规格或纯度	≥99%
英文名称	Tenofovir
别名	(R)-[[2-(6-氨基-9H-嘌呤-9-基)-1-甲基乙氧基]甲基]膦酸；(R)-9-(2-膦酰乙氧基丙基)腺嘌呤
英文别名	(R)-[[2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]phosphonic Acid；(R)-PMPA
生化机理	选择性抑制HIV逆转录酶（RNA依赖性DNA聚合酶）。预防SIV感染的C-8166细胞在体外的细胞毒性（IC50 =1.5μM）。抗病毒剂。
储存温度	-20°C储存
运输条件	超低温冰袋运输

名称和标识符

IUPAC Name	[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid
INCHI	InChI=1S/C9H14N5O4P/c1-6(18-5-19(15,16)17)2-14-4-13-7-8(10)11-3-12-9(7)14/h3-4,6H,2,5H2,1H3,(H2,10,11,12)(H2,15,16,17)/t6-/m1/s1
InChi Key	SGOIRFVFHAKUTI-ZCFIWIBFSA-N
Canonical SMILES	CC(CN1C=NC2=C(N=CN=C21)N)OCP(=O)(O)O
分子式	C₉H₁₄N₅O₄P
关联CAS	206184-49-8
PubChem CID	464205
分子量	287.22

数据库链接

CAS Registry No.	147127-20-6
RCSB PDB Ligand	TFO
PubChem CID	464205
ChEBI	CHEBI:63625
ChEMBL Ligand	CHEMBL483
DrugBank Ligand	DB14126
DrugCentral Ligand	2592

化学和物理性质

溶解性	溶于1.1eq. NaOH, 最高浓度 (mg/mL): 28.72, 最高浓度(mM): 100；溶于DMSO, 最高浓度 (mg/mL): 2.87, 最高浓度(mM): 10
敏感性	对热敏感
熔点	283 °C
比旋光度	-20° (C=1,0.1mol/L HCl)

安全信息

象形图	Corrosive
信号词	Danger
危险声明	H318: Causes serious eye damage
预防措施声明	P280,P264+P265,P305+P354+P338,P317
Merck Index	9146

关联配体

Ligand ID	10948
名称	tenofovir
别名	PMPA
类别	Synthetic organic
学名	[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid
生物活性评价	OAT1 and OAT3 in the basal membrane actively transport 20-30% of tenofovir into proximal tubule cells . ABCC2 (MRP2) and ABCC4 (MRP4) at the apical surface secrete tenofovir into the tubular lumen .
评价	Tenofovir is a nucleotide reverse transcriptase inhibitor (NtRTI) antiretroviral compound. The R-enantiomer, as shown here, is more effective at inhibiting retroviruses than the S-enantiomer . Tenofovir has poor oral bioavailability and is delivered as either the prodrug tenofovir disoproxil fumarate (Viread®) or tenofovir alafenamide fumerate (Vemlidy®).
临床描述	Healthcare workers are particularly at risk of SARS-CoV-2. This study aims to assess the efficacy of a daily single dose of tenofovir disoproxil fumarate (TDF) (245 mg)/ Emtricitabine (FTC) (200 mg), a daily single dose of hydroxychloroquine (HC) (200 mg), a daily single dose of TDF (245 mg)/FTC (200 mg) plus HC (200 mg) versus placebo, during 12 weeks in: (1) reducing the incidence of symptomatic disease and (2) reducing clinical severity COVID-19 among hospital healthcare workers aged 18 to 70 years in public and private hospitals in Spain. Effectiveness of the use of Tenofovir/Emtricitabine in addition to personal protective equipment for the prevention of the transmission of SARS-COV-2 to health care personnel. A Randomized Clinical Trial. This is an experimental study whose aim is to evaluate the effectiveness of a drug to prevent infection with the virus that causes COVID-19 (SARS-CoV-2), in health care workers. The drug under study is Tenofovir /Emtricitabine, a well-known antiretroviral, which is safe and is used as prophylaxis and treatment for HIV and other viral infections such as Hepatitis. Several laboratory-based studies indicate that this drug has the potential to inhibit SARS-CoV-2 replication. In addition, one study in HIV infected persons found that those taking Tenofovir /Emtricitabine tended to have a lower occurrence of COVID-19. In this study, we will compare the occurrence of infection with SARS-CoV-2/ COVID19 in health care workers between those assigned to an intervention group and those assigned to a control group. The intervention group will receive Tenofovir /Emtricitabine during 60 days in addition to the use of personal protective equipment (PPE), and the control group will receive a placebo during 60 days in addition to the use of personal protective equipment (PPE). The study will recruit 950 health professionals above 18 and less than 70 years, working in the emergency room, COVID wards and intensive care units of seven hospitals in Colombia. To make the comparison groups very similar, the participants will be assigned through a random mechanism to either the intervention (475), or the control (475) groups. In order to prevent biases in the evaluation of the results, neither the participants nor the clinical investigators, data managers, analysts and support personnel will know which intervention the participants are receiving. To determine the occurrence of infection with the virus the study will use both molecular tests that detect the presence of viral genes in respiratory secretions, and serological tests that detect the response of the immune system to the virus. The study will evaluate also the safety of this drug determining the occurrence of adverse events. A randomized parallel double-blinded placebo-controlled clinical trial to evaluate the effect of Emtricitabine/Tenofovir alafenamide (FTC/TAF) compared with placebo on the risk of developing SARS-CoV-2 disease (COVID-19) in healthcare workers with high transmission risk in addition to currently recommended control measures.
来源公司	Plan Nacional sobre el Sida (PNS) Hospital Universitario San Ignacio Hospital Italiano de Buenos Aires

参考文献

1. Cooper RD, Wiebe N, Smith N, Keiser P, Naicker S, Tonelli M. (2010) Systematic review and meta-analysis: renal safety of tenofovir disoproxil fumarate in HIV-infected patients.. Clin Infect Dis, 51 (5): (496-505). [PMID:20673002]
2. Fernandez-Fernandez B, Montoya-Ferrer A, Sanz AB, Sanchez-Ni?o MD, Izquierdo MC, Poveda J, Sainz-Prestel V, Ortiz-Martin N, Parra-Rodriguez A, Selgas R et al.. (2011) Tenofovir nephrotoxicity: 2011 update.. AIDS Res Treat, 2011 (13): (354908). [PMID:21716719]
3. Kalyesubula R, Perazella MA. (2011) Nephrotoxicity of HAART.. AIDS Res Treat, 2011 (13): (562790). [PMID:21860787]
4. Zaidan M, Lescure FX, Brochériou I, Dettwiler S, Guiard-Schmid JB, Pacanowski J, Rondeau E, Pialoux G, Girard PM, Ronco P et al.. (2013) Tubulointerstitial nephropathies in HIV-infected patients over the past 15 years: a clinico-pathological study.. Clin J Am Soc Nephrol, 8 (6): (930-8). [PMID:23430209]
5. Balzarini J, Holy A, Jindrich J, Naesens L, Snoeck R, Schols D, De Clercq E. (1993) Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine.. Antimicrob Agents Chemother, 37 (2): (332-8). [PMID:8452366]

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