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/ Raltegravir

雷特格韦 /Raltegravir {[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 化学结构 CAS号：518048-05-0
Raltegravir 化学结构
CAS号：518048-05-0
Raltegravir 3D分子结构
CAS号：518048-05-0
Raltegravir 化学结构 CAS号：518048-05-0
Raltegravir 3D分子结构 CAS号：518048-05-0
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Raltegravir 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]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]
• JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]
• BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]
• J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]
• PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]
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Raltegravir 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 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 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 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 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 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 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 技术信息

CAS号518048-05-0
分子式C20H21FN6O5
分子量 444.416
别名 雷特格韦 (MK-0518) ;MK-0518
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C
溶解度

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
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 纯度/质量文件 | Raltegravir 生物活性 | Raltegravir 细胞研究 | Raltegravir 动物研究 | Raltegravir 临床数据 | Raltegravir 参考文献 | Raltegravir 实验方案 | Raltegravir 技术信息

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