Efavirenz (DMP 266) 是一种有效的野生型 HIV-1 RT 抑制剂，Ki 为 2.93 nM，抑制 HIV-1 复制，IC95 为 1.5 nM。
| 生物活性 |
Efavirenz (DMP 266) 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. |
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| 体外研究 |
Efavirenz (L-743726) is found to be capable of inhibiting, with 95% inhibitory concentrations of ≤ 1.5μM, a panel of nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs)-resistant mutant viruses, each of which expresses a single RT amino acid substitution. Efavirenz is also tested for its activity against a variety of polymerase enzymes and is found to be inactive (IC50>300μM). Efavirenz effectively inhibits several wild-type T-lymphoid cell line-adapted variants. Identical activity (IC95, 1.5 to 3.0 nM) is seen with wild-type primary isolates of the virus in both primary lymphoid and monocytoid cell cultures. Efavirenz also effectively inhibits HIV-1 variants that expressed RT amino acid substitutions which confer the loss of susceptibility to other NNRTIs. For purposes of comparison. Efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI) with IC50 of 60 nM. Efavirenz inhibits synthesis using an RNA PPT-primed substrate with an IC50 of 17 nM. |
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| 体内研究 |
After i.v. administration, Efavirenz (L-743726) is cleared rapidly from rats, but it is cleared considerably more slowly from monkeys. The large volume of distribution (two to four times the amount of body water) in both species indicates extensive tissue binding. The oral bioavailability in rats is 16%. In monkeys, the half-life of Efavirenz after administration of a 1 mg/kg i.v. dose exceeded 2.5 h. Efavirenz is well absorbed orally. Administration to monkeys of oral doses as fine suspensions in 0.5% aqueous methylcellulose yields consistently high levels in plasma. A 2.0 mg/kg dose produces peak levels of 0.5μM at approximately 3.0 h. The absolute bioavailability is estimated to be 42%. A 10 mg/kg dose yields a peak level in plasma of 3.22 μM. A 10 mg/kg oral dose given to a single chimpanzee gave concentrations in plasma of 4.12, 2.95, and 2.69 μM at 2, 8, and 24 h after dosing, respectively.
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| 分子式 |
C14H9ClF3NO2
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| 分子量 |
315.68
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| CAS号 |
154598-52-4
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| 中文名称 |
依法韦仑；施多宁；依法韦伦；依法维仑；依氟维纶；依非韦伦；艾法韦仑
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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| 溶解性数据 |
In Vitro:
DMSO : ≥ 38 mg/mL (120.38 mM) * "≥" means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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| 临床试验 |
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| 科研文献 |
纯度： 98%
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Data Sheet
