[CAS NO. 1051375-19-9] Dolutegravir Sodium

Name: Dolutegravir Sodium
Brand: Arctom Scientific
SKU: SLK-S4642

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PRODUCTS SPECIFICATIONS [1051375-19-9]

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Catalog

SLK-S4642

Brand

Selleck

CAS

1051375-19-9

DESCRIPTION [1051375-19-9]

Overview

MDL	-
Molecular Weight	441.36
Molecular Formula	C20H19F2N3O5.Na
SMILES	O=C1C=2N(C[C@]3(N1[C@H](C)CCO3)[H])C=C(C(NCC4=C(F)C=C(F)C=C4)=O)C(=O)C2O.[Na]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2657 mL	11.3286 mL	22.6572 mL
5 mM	0.4531 mL	2.2657 mL	4.5314 mL
10 mM	0.2266 mL	1.1329 mL	2.2657 mL
50 mM	-	-	-

Description

Dolutegravir Sodium (GSK-1349572A) is a inhibitor with of 2.7 nM.

Targets

HIV integrase ^[1]
(Cell-free assay)

2.7 nM

In vitro

Dolutegravir(S/GSK1349572) inhibits HIV-1 integrase-catalyzed strand transfer with a 50% inhibitory concentration (IC50) of 2.7 nM. S/GSK1349572 inhibits both the HIV integration reaction strand transfer step in vitro and HIV replication in cells with similar potencies. The inhibitor has no effect on total viral DNA synthesis in infected cells but blocks the integration of viral DNA into host DNA with the same potency as its antiviral effect.

In vivo

The bioavailability of dolutegravir was high when administered as a solution, but was limited by dissolution rate or solubility when administered as a suspension. Dolutegravir is the major circulating component in mice, rats, and monkeys, with direct ether glucuronidation shown to be the primary biotransformation pathway. Dolutegravir is primarily eliminated via the feces either unabsorbed or by hydrolysis of the glucuronide or glucose conjugate.

References

[1] Kobayashi M, et al. Antimicrob Agents Chemother. 2011, 55(2):813-21.
[2] Moss L, et al. Xenobiotica. 2015, 45(1):60-70.

Synonyms

2H-Pyrido[1′,2′:4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide, N-[(2,4-difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-, sodium salt (1:1), (4R,12aS)-

Dolutegravir sodium

GSK 1349572A

Dolutegravir sodium salt