1. Anti-infection
    Metabolic Enzyme/Protease
    Apoptosis
  2. HIV Protease
    HIV
    SARS-CoV
    Apoptosis
  3. Ritonavir

Ritonavir (Synonyms: 利托那韦; ABT 538; RTV)

目录号: HY-90001 纯度: 99.95%
产品使用指南

Ritonavir (ABT 538) 是用于研究 HIV 感染和 AIDS 的 HIV 蛋白酶的抑制剂。Ritonavir 也是 SARS-CoV 3CLpro 的抑制剂,IC50 为 1.61 μM。

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Ritonavir Chemical Structure

Ritonavir Chemical Structure

CAS No. : 155213-67-5

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥517 In-stock
10 mg ¥470 In-stock
50 mg ¥1100 In-stock
100 mg ¥1900 In-stock
500 mg ¥5500 In-stock
1 g   询价  
5 g   询价  

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Other Forms of Ritonavir:

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  • 生物活性

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  • 参考文献

生物活性

Ritonavir (ABT 538) is an inhibitor of HIV protease used to treat HIV infection and AIDS. Ritonavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 1.61 μM.

体外研究
(In Vitro)

Ritonavir (ABT 538) is an inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM[1]. Ritonavir (ABT 538) is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 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 IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein[4]. Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

720.94

Formula

C₃₇H₄₈N₆O₅S₂

CAS 号
中文名称

利托那韦;瑞托纳韦

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

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

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.3871 mL 6.9354 mL 13.8708 mL
5 mM 0.2774 mL 1.3871 mL 2.7742 mL
10 mM 0.1387 mL 0.6935 mL 1.3871 mL
*

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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

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
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-CD in 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 μL 20% 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-CD in 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

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

Purity: 99.95%

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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