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/ Raltegravir/雷特格韦

Raltegravir/雷特格韦 {[allProObj[0].p_purity_real_show]}

货号：A121488 同义名： 雷特格韦 (MK-0518) / MK-0518

Raltegravir是一种强力的整合酶（IN）抑制剂，用于治疗HIV感染。

Raltegravir/雷特格韦 化学结构 CAS号：518048-05-0
Raltegravir/雷特格韦 化学结构
CAS号：518048-05-0
Raltegravir/雷特格韦 3D分子结构
CAS号：518048-05-0
Raltegravir/雷特格韦 化学结构 CAS号：518048-05-0
Raltegravir/雷特格韦 3D分子结构 CAS号：518048-05-0
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Raltegravir/雷特格韦 纯度/质量文件 产品仅供科研

货号：A121488 标准纯度： {[allProObj[0].p_purity_real_show]}
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Raltegravir/雷特格韦 生物活性

描述 Raltegravir is the first approved clinical used inhibitor of integrase which can inhibit different kind of INs with alternative IC50 values, for example, the IC50 for the wild type and S217Q prototype foamy virus(PFV) IN are 90 nM and 40 nM respectively, while it’s 3.3 nM for HIV IN. In human MT-4 cells, the IC50 for raltegravir to inhibit overall IN activity was 9nM while it inhibited strand transfer step at 6.8nM. Besides, this compound could reduce HIV-1-induced CPE by 50% at the concentration of 1.4nM. At the concentration of >18 μM, MT-4 cells viability could be inhibited, suggesting a good antiviral activity for HIV. While MT-4 cells infected with SIVmac251, Raltegravir could inhibit SIVmac251 replication with a lower EC50 value (< 1nM) compared with HIV-1/HIV-2 infected MT-4 cells. In SIVmac251 infected CEMx174 cells, Raltegravir displayed reproducible anti-SIVmac251 activity by using of syncytia counts which could be still produced in the presence of this compound, while the syncytia formation induced apoptotic and necrotic cell death in MT-4 cells. In human CD4+ T cells, Raltegravir also showed inhibitory effect when the cell fraction showed expression of the CD4 antigen >94%. In one phase 2 study, 198 HIV-1 infected participants with the HIV-1 RNA level at >5000 copies/mL and the CD4 cell count >100 cells/μL were treated with 400 mg Raltegravir twice daily from 48 week. The result showed that the proportions of patients with an HIV-1 RNA level at <50 copies/mL were 83%. While in another phase 2 study, the 201 HIV-1 infected participants with the same RNA and CD4 levels were treated with gradient concentrations of Raltegravir twice daily showed a quicker reduction on RNA levels at week 48 that ranges in 83%-88% in a dose-independent manner.

Raltegravir/雷特格韦 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
human HeLa cells Function assay 48 h Antiviral activity against VSV-G pseudotyped HIV1 lentiviral particles infected in human HeLa cells incubated for 48 hrs by spectrofluorometry, IC50=10 nM 22858300
human HOS cells Function assay Antiviral activity against HIV1 harboring wild-type integrase infected in human HOS cells, EC50=4 nM 21493066
human MT2 cells Function assay 5 days Antiviral activity against HIV1 3B infected in human MT2 cells after 5 days by chemiluminescence in presence of fetal bovine serum, EC50=4 nM 19285389
human MT4 cells Function assay Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as inhibition of viral replication, EC50=1.4 nM 18541726

Raltegravir/雷特格韦 动物研究

Dose Rat: 40 mg/kg - 160 mg/kg[3] (intragastrically) Dog: 5 mg/kg - 135 mg/kg[4] (p.o.)
Administration Intragastrically
Pharmacokinetics
Animal Rats[4] Dogs[4]
Dose 6 mg/kg (p.o.)
3 mg/kg (i.v.) 		5 mg/kg (p.o.)
1.5 mg/kg (i.v.)
Administration p.o.
i.v. 		p.o.
i.v.
F 61.6% (p.o.) 70.0% (p.o.)
T1/2 0.2 h (i.v.) 1.6 h (i.v.)
Tmax 0.4 h (p.o.) 0.6 h (p.o.)
CLp 45.5 ml/h/kg (i.v.) 7.4 ml/h/kg (i.v.)
Cmax 1.7 μg/ml (p.o.) 11.9 μg/ml (p.o.)
Vdss 2.2 L/kg (i.v.) 0.4 L/kg (i.v.)
AUC0→∞ 3.2 μM·h (p.o.)
2.6 μM·h (i.v.) 		18.6 μM·h (p.o.)
7.9 μM·h (i.v.)

Raltegravir/雷特格韦 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
NCT01270802 HIV Phase 4 Completed - United States, Indiana ... 展开 >> Indiana University School of Medicine Indianapolis, Indiana, United States, 46202 收起 <<
NCT00654147 HIV Infections Phase 2 Completed - United States, Florida ... 展开 >> University of Miami AIDS Clinical Research Unit Miami, Florida, United States, 33136 收起 <<
NCT01270802 - Completed - -

Raltegravir/雷特格韦 参考文献

[1]Zhang X, Huang H, et al. Raltegravir Attenuates Experimental Pulmonary Fibrosis In Vitro and In Vivo. Front Pharmacol. 2019 Aug 20;10:903.

[2]Raltegravir

Raltegravir/雷特格韦 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.25mL

2.25mL

1.13mL

22.50mL

4.50mL

2.25mL

Raltegravir/雷特格韦 技术信息

CAS号518048-05-0
分子式C20H21FN6O5
分子量 444.42
SMILES Code O=C1C(O)=C(N=C(N1C)C(C)(NC(C2=NN=C(O2)C)=O)C)C(NCC3=CC=C(C=C3)F)=O
MDL No. MFCD10698872
别名 雷特格韦 (MK-0518) ;MK-0518
运输蓝冰
InChI Key CZFFBEXEKNGXKS-UHFFFAOYSA-N
Pubchem ID 54671008
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C
溶解方案

DMSO: 105 mg/mL(236.26 mM)，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
动物实验配方

2% DMSO+40% PEG 300+2% Tween 80+water 8 mg/mL

Tags: Raltegravir | 518048-05-0 | MK-0518 | MK0518 | MK 0518 | Integrase Inhibitor | Metabolic Enzyme/Protease | Anti-infection | HIV Integrase | HIV | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Raltegravir/雷特格韦 纯度/质量文件 | Raltegravir/雷特格韦 生物活性 | Raltegravir/雷特格韦 细胞研究 | Raltegravir/雷特格韦 动物研究 | Raltegravir/雷特格韦 临床数据 | Raltegravir/雷特格韦 参考文献 | Raltegravir/雷特格韦 实验方案 | Raltegravir/雷特格韦 技术信息

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