Ritonavir (ABT 538) is an inhibitor ofHIV proteaseused to treat HIVinfectionand AIDS. Ritonavir is also aSARS-CoV3CL^proinhibitor with anIC₅₀of 1.61 μM.

Ritonavir (ABT 538) is an inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean K_iof 19 nM and also inhibits tolbutamide hydroxylation with IC₅₀of 4.2 μM^[1]. Ritonavir (ABT 538) is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC₅₀of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC₅₀of 2 mM; terfenadine hydroxylation with IC₅₀of 0.14 mM). Ritonavir is also an inhibitor of the reactions mediated by CYP2D6 (IC₅₀=2.5 mM) and CYP2C9/10 (IC₅₀=8.0 mM)^[2]. Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations^[3]. Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC₅₀of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein^[4]. Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with K_iof 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC₅₀=1.1 and 4.6 μM), albeit less potently than Ritonavir (IC₅₀=0.14 μM)^[5].

720.94

Solid

C₃₇H₄₈N₆O₅S₂

155213-67-5

利托那韦；瑞托纳韦

Room temperature in continental US; may vary elsewhere.

DMSO : 25 mg/mL(34.68 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

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    90% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (3.47 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 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
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: 2.5 mg/mL (3.47 mM); Clear solution; Need warming

  此方案可获得 2.5 mg/mL (3.47 mM) 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• 3.

  请依序添加每种溶剂： 5% DMSO    40%PEG300   5%Tween-80   50% saline

  Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
• 4.

  请依序添加每种溶剂： 5% DMSO    95% (20%SBE-β-CDin saline)

  Solubility: 2.5 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
• 5.

  请依序添加每种溶剂： 1% DMSO    99% saline

  Solubility: 0.5 mg/mL (0.69 mM); Suspended solution; Need ultrasonic