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/ Efavirenz

依法韦仑 /Efavirenz {[allProObj[0].p_purity_real_show]}

货号：A909233 同义名： 依非韦伦 / DMP 266;EFV

Efavirenz is an inhibitor of wild-type HIV-1 reverse transcriptase with Ki of 2.93 nM and the IC95 of its replicative spread is 1.5 nM in cell culture.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Efavirenz 化学结构 CAS号：154598-52-4
Efavirenz 化学结构
CAS号：154598-52-4
Efavirenz 3D分子结构
CAS号：154598-52-4
Efavirenz 化学结构 CAS号：154598-52-4
Efavirenz 3D分子结构 CAS号：154598-52-4
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Efavirenz 纯度/质量文件 产品仅供科研

货号：A909233 标准纯度： {[allProObj[0].p_purity_real_show]}
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Efavirenz 生物活性

描述 Efavirenz is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[3]. Efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI) with IC50 of 60 nM[4]. Efavirenz inhibits synthesis using an RNA PPT-primed substrate with an IC50 of 17 nM[5]. Efavirenz is administered once-daily and its simple dosing schedule improves adherence to therapy allowing for durability of the virologic and clinical responses[6]. Efavirenz exerts a lysergide (LSD)-like effect on brain serotonergic pathways and affects CNS metabolic pathways, including mitochondrial function[7].

Efavirenz 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01837277 Severely Immunocompromised HIV... 展开 >> Patients 收起 << Phase 2 Phase 3 Unknown March 2016 Brazil ... 展开 >> Fundação Bahiana de Infectologia/SEI Not yet recruiting Salvador, Bahia, Brazil, 40010-160 Contact: Estela Luz, RN, MSci    32838123    eluz5@yahoo.com.br    Principal Investigator: Carlos Brites, MD, PhD          Sub-Investigator: Fabianna Bahia, MD, PhD          Universidade Federal do Rio de Janeiro Not yet recruiting Rio de Janeiro, RJ, Brazil Contact: Monica Ponze, RN    5521222739073       Principal Investigator: Mauro Schechter, MD, PhD          Hospital de Clinicas de Porto Alegre Not yet recruiting Porto Alegre, RS, Brazil Contact: Priscila Pelaez, MD          Principal Investigator: Eduardo Sprinz, MD, PhD 收起 <<
NCT00002227 HIV Infections Phase 2 Completed - United States, District of Col... 展开 >>umbia Richard Elion Washington, District of Columbia, United States, 20009 The Whitman Walker Clinic Washington, District of Columbia, United States, 20009 United States, Massachusetts Community Research Initiative of New England Brookline, Massachusetts, United States, 02445 United States, Ohio Remington Davis Inc Columbus, Ohio, United States, 43215 United States, Pennsylvania The Milton S Hersey Med Ctr / Div of Hematology Hershey, Pennsylvania, United States, 170330850 United States, South Carolina Coastal Carolina Research Ctr Mount Pleasant, South Carolina, United States, 29464 United States, Texas Montrose Clinic Houston, Texas, United States, 77006 United States, Virginia Hampton Roads Med Specialists Hampton, Virginia, United States, 23666 收起 <<
NCT00002225 HIV Infections Phase 2 Completed - United States, District of Col... 展开 >>umbia The Whitman Walker Clinic Washington, District of Columbia, United States, 20009 United States, Illinois AIDS Research Alliance - Chicago Chicago, Illinois, United States, 60657 United States, New York North Shore AIDS Hosp / Division of Infectious Disease Manhassett, New York, United States, 11030 Univ of Rochester Med Ctr Rochester, New York, United States, 14642 United States, North Carolina Carolinas Research Associates Charlotte, North Carolina, United States, 28207 收起 <<

Efavirenz 参考文献

[1]Held DM, Kissel JD, et al. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22.

[2]Young SD, Britcher SF, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5.

[3]Young SD, Britcher SF, Tran LO, Payne LS, Lumma WC, Lyle TA, Huff JR, Anderson PS, Olsen DB, Carroll SS, et al. L-743, 726 (DMP-266): a novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptase. Antimicrob Agents Chemother. 1995 Dec;39(12):2602-5

[4]Held DM, Kissel JD, Saran D, Michalowski D, Burke DH. Differential susceptibility of HIV-1 reverse transcriptase to inhibition by RNA aptamers in enzymatic reactions monitoring specific steps during genome replication. J Biol Chem. 2006 Sep 1;281(35):25712-22

[5]Grobler JA, Dornadula G, Rice MR, Simcoe AL, Hazuda DJ, Miller MD. HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro. J Biol Chem. 2007 Mar 16;282(11):8005-10

[6]Maggiolo F. Efavirenz. Expert Opin Pharmacother. 2007 Jun;8(8):1137-45

[7]Van de Wijer L, Schellekens AFA, Burger DM, Homberg JR, de Mast Q, van der Ven AJAM. Rethinking the risk-benefit ratio of efavirenz in HIV-infected children. Lancet Infect Dis. 2016 May;16(5):e76-e81

Efavirenz 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.17mL

0.63mL

0.32mL

15.84mL

3.17mL

1.58mL

31.68mL

6.34mL

3.17mL

Efavirenz 技术信息

CAS号154598-52-4
分子式C14H9ClF3NO2
分子量 315.675
别名 依非韦伦 ;DMP 266;EFV;United Drug brand of efavirenz;Merck Sharp and Dohme brand of efavirenz;Stocrin;Sustiva;L-743726
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

DMSO: 40 mg/mL(126.71 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Efavirenz | DMP 266;EFV;United Drug brand of efavirenz;Merck Sharp and Dohme brand of efavirenz;Stocrin;Sustiva;L-743726 | 依非韦伦 | Drug Standard | Antivirus | Reverse Transcriptase Inhibitor | HIV | Reverse Transcriptase | NNRTI | AmBeed-信号通路专用抑制剂 | Efavirenz 纯度/质量文件 | Efavirenz 生物活性 | Efavirenz 临床数据 | Efavirenz 参考文献 | Efavirenz 实验方案 | Efavirenz 技术信息

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