Product Name: Dolutegravir(S/GSK1349572)
CAS No.1051375-16-6
Information: HIV integrase inhibitor, novel and potent
Description: Dolutegravir (GSK1349572) is an inhibitor of two-metal-binding HIV integrase with an IC50 value of 2.7 nM.
Other Names: S/GSK1349572, GSK-1349572
Chemical Name: (4R,12aS)-N-[(2,4-difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide
Canonical SMILES: CC1CCOC2N1C(=O)C3=C(C(=O)C(=CN3C2)C(=O)NCC4=C(C=C(C=C4)F)F)O
MF: C20H19N3O5F2
MW: 419.37876
Assay: 99% min
Type: Anti-HIV Agents
Grade Standard: Medicine Grade
Brand Name: Huavet
Solubility Soluble in DMSO > 10 mM
Storage: Store at -20°C
General tips: For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition: Evaluation sample solution: ship with blue ice. All other available size: ship with RT , or blue ice upon request
Background: Dolutegravir(S/GSK1349572), also known as dolutegravir, is a novel and potent inhibitor of human immunodeficiency virus (HIV) integrase (IN) blocking the strand transfer of integration of the viral genome into the host cell’s DNA. It occupies the physical space in the IN active site of the intasome, contacts with the β4-α2 loop of the catalytic core domain, and enters into the pocket vacated by the displaced viral DNA through its extended linker region connecting the metal chelating core the halobenzyl group. S/GSK1349572 exhibits potent anti-HIV activity in peripheral blood mononuclear cells (IC50 = 0.51 nM) in vitro and retains activity against raltegravir- and elvitegravir- resistant HIV.
Reference
Sherene Min, Ivy Song, Julie Borland, Shuguang Chen, Yu Lou, Tamio Fujiwara, and Stephen C. Piscitelli. Pharmacokinetics and safety of S/GSK1349572, a next-generation HIV integrase inhibitor, in healthy volunteers. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 2010; 54(1): 254-258
Masanori Kobayashi, Tomokazu Yoshinaga, Takahiro Seki, Chiaki Wakasa-Morimoto, Kevin W. Brown, Robert Ferris, Scott A. Foster, Richard J. Hazen, Shigeru Miki, Akemi Suyama-Kagitani, Shinobu Kawauchi-Miki, Teruhiko Taishi, Takashi Kawasuji, Brian A. Johns, Mark R. Underwood, Edward P. Garvey, Akihiko Sato, and Tamio Fujiwara. In vitro antiretroviral prooerties of S/GSK1349572, a next-generation HIV integrase inhibitor. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY 2011; 55(2): 813-821
Stephen Harem Steven J. Smith, Mathieu Metifiot, Albert Jaxa-Chamiec, Yves Pommier, Stephen H. Hughes, and Peter Cherepanov. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol 2011; 80(4): 565-572
Usage: Pharmaceutical Intermediates
Inventory status: in stock
Shelf life: 2 years
Sample: Available
COA (Certificate Of Analysis): Available
MSDS (Material Safety Data Sheet): Available
HPLC Spectrum: Available
ISO: Approved
GC: Available
NMR (Nuclear Magnetic Resonance): Available
Packaging Details: 1g,5g,10g,50g,100g/bottle, 1kg/tin for trial order,25kg/drum for commercial quantity. Specific packing required by customer
Delivery Detail: Prompt shipment
