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/ Cabotegravir

卡博特韦 /Cabotegravir {[allProObj[0].p_purity_real_show]}

货号：A115208 同义名： GSK-1265744;S/GSK1265744

Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).

Cabotegravir 化学结构 CAS号：1051375-10-0
Cabotegravir 化学结构
CAS号：1051375-10-0
Cabotegravir 3D分子结构
CAS号：1051375-10-0
Cabotegravir 化学结构 CAS号：1051375-10-0
Cabotegravir 3D分子结构 CAS号：1051375-10-0
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Cabotegravir 纯度/质量文件 产品仅供科研

货号：A115208 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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Cabotegravir 生物活性

描述 Cabotegravir (GSK-1265744) operates as an orally available, long-acting inhibitor of the HIV integrase strand transfer and the organic anion transporters 1 and 3 (OAT1/OAT3), with IC50s of 2.5 nM for HIVADA, 0.41 μM for OAT3, and 0.81 μM for OAT1. Its metabolism is mainly via the uridine diphosphate glucuronosyltransferase (UGT) 1A1, presenting minimal interaction risks with other antiretroviral drugs (ARVs), making it suitable for AIDS researc[1].[2].
体内研究

Cabotegravir administered intravenously at doses of either 25 or 50 mg/kg, once or twice, effectively shields Macaques from an intravenous SIVmac251 challenge[4].
体外研究

Cabotegravir (GSK-1265744) inhibits the HIV-1 integrase catalyzed strand transfer reaction with an IC50 of 3.0 nM in vitro.It shows antiviral activity with EC50 values ranging from 0.22 nM to 1.3 nM against various HIV-1 strains in different cellular assays. Additionally, it effectively shields Macaques from intravenous SIVmac251 challenges when administered as a single or double dose of 25 or 50 mg/kg intravenously[3].

Cabotegravir 动物研究

Dose Rhesus macaques: 10 mg/kg - 50 mg/kg[3] (i.m.)
Administration i.m.

Cabotegravir 参考文献

[1]Zhou T, et al. Creation of a nanoformulated cabotegravir prodrug with improved antiretroviral profiles. Biomaterials. 2018 Jan;151:53-65.

[2]Reese MJ, et al. Drug interaction profile of the HIV integrase inhibitor cabotegravir: assessment from in vitro studies and a clinical investigation with midazolam. Xenobiotica. 2015 Sep 4:1-12.

[3]Yoshinaga T, et al. Antiviral characteristics of GSK1265744, an HIV integrase inhibitor dosed orally or by long-acting injection. Antimicrob Agents Chemother. 2015 Jan;59(1):397-406.

[4]Andrews CD, et al. Cabotegravir long acting injection protects macaques against intravenous challenge with SIVmac251. AIDS. 2017 Feb 20;31(4):461-467.

Cabotegravir 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.33mL

2.47mL

1.23mL

24.67mL

4.93mL

2.47mL

Cabotegravir 技术信息

CAS号1051375-10-0
分子式C19H17F2N3O5
分子量 405.352
别名 GSK-1265744;S/GSK1265744;GSK1265744A;GSK744
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,Room Temperature
溶解度

DMSO: 16 mg/mL(39.47 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
动物实验配方

Tags: Cabotegravir | GSK-1265744;S/GSK1265744;GSK1265744A;GSK744 | HIV Integrase | HIV | AmBeed-信号通路专用抑制剂 | Cabotegravir 纯度/质量文件 | Cabotegravir 生物活性 | Cabotegravir 动物研究 | Cabotegravir 参考文献 | Cabotegravir 实验方案 | Cabotegravir 技术信息

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