Darunavir Ethanolate

Catalogue Number: B4950-APE

Manufacturer:	Apexbio
Molecular Formula:	C29H43N3O8S
Physical state:	A solid
Type:	Protease Inhibitors
Shipping Condition:	Blue Ice
Unit(s):	10 mM (in 1mL DMSO), 5 mg, 50 mg

Overview
Datasheets

Description

Description: 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.

Additional Text

Storage Note

Store at -20°C

Short Description

nonpeptidic HIV protease inhibitor

Reagent:Smile String

O[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

Solubility

≥59.17 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O

B4950 CofA

B4950 MSDS

Price

£101.00

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