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Ritonavir/利托那韦 {[allProObj[0].p_purity_real_show]}

货号:A547820 同义名: ABT 538; RTV

Ritonavir是HIV蛋白酶抑制剂,也是细胞色素P450 3A抑制剂。

Ritonavir/利托那韦 化学结构 CAS号:155213-67-5
Ritonavir/利托那韦 化学结构
CAS号:155213-67-5
Ritonavir/利托那韦 3D分子结构
CAS号:155213-67-5
Ritonavir/利托那韦 化学结构 CAS号:155213-67-5
Ritonavir/利托那韦 3D分子结构 CAS号:155213-67-5
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Ritonavir/利托那韦 纯度/质量文件 产品仅供科研

货号:A547820 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 HIV Protease HIV-1 caspid 其他靶点 纯度
Dextran sulfate sodium salt(MW 40000) M.W 40000
Vicriviroc maleate 95%
Rosamultin 97%
Darunavir 98%
Lopinavir ++++

HIV protease, Ki: 1.3 pM

99+%
Chloroquine Autophagy 95%
Amprenavir +

HIV protease, IC50: 14.6 ng/mL

PXR 99%+
NBD-556 99%+
Nelfinavir Mesylate +++

HIV protease, Ki: 2 nM

99%+
Atazanavir Sulfate 98%
Limonin 98%
Saquinavir ++

HIV proteinase, IC50: 2.7 nM

98%
Ritonavir 98%
Azvudine 98%
Lenacapavir ++++

HIV-1 capsid, EC50: 0.1 nM

97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Ritonavir/利托那韦 生物活性

靶点
  • HIV Protease

描述 Ritonavir is n antiretroviral medication used along with other medications to treat HIV/AIDS. It is now rarely used for its own antiviral activity, but remains widely used as a booster of other protease inhibitors. More specifically, ritonavir is used to inhibit a particular liver enzyme that normally metabolizes protease inhibitors, cytochrome P450-3A4 (CYP3A4) [3]. The HIV-1 protease inhibitor ritonavir undergoes cytochrome P450-mediated biotransformation in human liver microsomes to three major metabolites, Ml, M2 and M11, with wide interindividual variation in the rates of metabolite formation. Ritonavir was found to be a potent inhibitor of CYP3A-mediated biotransformations. Ritonavir was also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 microM) and CYP2C9/10 (IC50 = 8.0 microM) [4].

Ritonavir/利托那韦 细胞实验

Cell Line
Concentration Treated Time Description References
GBM-P1 primary human glioblastoma cells 45 μM 72 hours Test the inhibitory effect of RTV on primary glioblastoma cell proliferation, found that 45 μM RTV consistently inhibited cell proliferation Neoplasia. 2017 Apr;19(4):364-373.
Hu197 human glioblastoma cells 45 μM 72 hours Test the inhibitory effect of RTV on Hu197 cell proliferation, found that 45 μM RTV consistently inhibited cell proliferation Neoplasia. 2017 Apr;19(4):364-373.

Ritonavir/利托那韦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BlC mice GL261 glioblastoma model Intraperitoneal injection 100 mg/kg 24 hours Test the therapeutic effect of RTV combined with BCNU on the GL261 glioblastoma model, found that the combination significantly prolonged mouse survival, and there was no significant difference between 1 mg/kg and 2.5 mg/kg BCNU Neoplasia. 2017 Apr;19(4):364-373.

Ritonavir/利托那韦 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
NCT00775606 - Terminated(Study stopped 12/20... 展开 >>10 due to poor enrollment. Only 15 of 60 needed enrolled.) 收起 << - -
NCT01346982 HIV Phase 4 Completed - Spain ... 展开 >> Lluita contra la Sida Foundation, HIV Unit Badalona, Barcelona, Spain, 08916 收起 <<
NCT00744887 HIV AIDS Phase 1 Completed - -

Ritonavir/利托那韦 参考文献

[1]Eagling VA, Back DJ, et al. Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. Br J Clin Pharmacol. 1997 Aug;44(2):190-4.

[2]Kumar GN, Rodrigues AD, et al. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31.

[3]Zeldin RK, Petruschke RA. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients. J Antimicrob Chemother. 2004 Jan;53(1):4-9. doi: 10.1093/jac/dkh029. Epub 2003 Dec 4. PMID: 14657084.

[4] Kumar GN, Rodrigues AD, Buko AM, Denissen JF. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir (ABT-538) in human liver microsomes. J Pharmacol Exp Ther. 1996 Apr;277(1):423-31. Erratum in: J Pharmacol Exp Ther 1997 Jun;281(3):1506. PMID: 8613951.

Ritonavir/利托那韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.94mL

1.39mL

0.69mL

13.87mL

2.77mL

1.39mL

Ritonavir/利托那韦 技术信息

CAS号155213-67-5
分子式C37H48N6O5S2
分子量 720.94
SMILES Code O=C(N[C@@H](CC1=CC=CC=C1)[C@H](C[C@H](CC2=CC=CC=C2)NC([C@H](C(C)C)NC(N(CC3=CSC(C(C)C)=N3)C)=O)=O)O)OCC4=CN=CS4
MDL No. MFCD00927142
别名 ABT 538; RTV; 538, ABT; Norvir Sec; Norvir; NSC 693184; A-84538
运输蓝冰
InChI Key NCDNCNXCDXHOMX-XGKFQTDJSA-N
Pubchem ID 392622
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 25 mg/mL(34.68 mM),配合低频超声助溶,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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
方案 二
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