产品说明书

Cabotegravir

Print
Chemical Structure| 1051375-10-0 同义名 : GSK-1265744;S/GSK1265744;GSK1265744A;GSK744
CAS号 : 1051375-10-0
货号 : A115208
分子式 : C19H17F2N3O5
纯度 : 98%
分子量 : 405.352
MDL号 : MFCD25976748
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.