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

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Cabotegravir/卡博特韦 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].

Cabotegravir/卡博特韦 动物研究

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

Cabotegravir/卡博特韦 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/卡博特韦 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

12.34mL

2.47mL

1.23mL

24.67mL

4.93mL

2.47mL

Cabotegravir/卡博特韦 技术信息

CAS号1051375-10-0
分子式C19H17F2N3O5
分子量 405.35
SMILES Code O=C(C1=CN(C2=C(O)C1=O)C[C@](OC[C@@H]3C)([H])N3C2=O)NCC4=CC=C(F)C=C4F
MDL No. MFCD25976748
别名 GSK-1265744; S/GSK1265744; GSK1265744A; GSK744
运输蓝冰
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

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