Efavirenz (DMP 266) is a potent inhibitor of the wild-typeHIV-1reverse transcriptasewith aK_iof 2.93 nM and exhibits anIC₉₅of 1.5 nM for the inhibition ofHIV-1replicative spread incell culture^[1].

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^[1]. Efavirenz is a non-nucleoside analog reverse transcriptase inhibitor (NNRTI) with IC₅₀of 60 nM^[2]. Efavirenz inhibits synthesis using an RNA PPT-primed substrate with an IC₅₀of 17 nM^[3].

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^[1].

315.68

Solid

C₁₄H₉ClF₃NO₂

154598-52-4

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

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 38 mg/mL(120.38 mM)

*"≥" means soluble, but saturation unknown.

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。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (6.59 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (6.59 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。