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Darunavir Ethanolate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Darunavir Ethanolate图片
CAS NO:635728-49-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
50mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt593.73
Cas No.635728-49-3
FormulaC29H43N3O8S
Solubility≥21 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
Chemical Name(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbamate compound with ethanol (1:1)
Canonical SMILESO[C@H](CN(CC(C)C)S(=O)(C(C=C1)=CC=C1N)=O)[C@H](CC2=CC=CC=C2)NC(O[C@@H]3[C@H]4[C@H](OCC4)OC3)=O.OCC
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

Darunavir ethanolate is a nonpeptidic HIV protease inhibitor approved for the treatment of HIV infection[1].

Transepithelial transport of darunavir in Caco-2 cell monolayers is 2-fold greater in the basal-to-apical direction compared to that in the opposite direction. In L-MDR1 cell, darunavir (121 mM) inhibits P-glycoprotein-mediated efflux of calcein-acetoxymethyl ester[1].

Darunavir is effective against wild-type and PI-resistant HIV, and has a low oral bioavailability (37%). When used in combination with ritonavir, bioavailability can be increased to 82%[2].

References:

[1]. Fujimoto H, Higuchi M, Watanabe H, et al. P-Glycoprotein Mediates Efflux Transport of Darunavir in Human Intestinal Caco-2 and ABCB1 Gene-Transfected Renal LLC-PK1 Cell Lines. Biological & Pharmaceutical Bulletin, 2009, 32(9): 1588-1593.

[2]. Bhalekar MR, et al. In-vivo bioavailability and lymphatic uptake evaluation of lipid nanoparticulates of darunavir. Drug Deliv, 2016, 23(7): 2581-2586.