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BMS-663068

Catalog No.
A3254
HIV-1 attachment inhibitor
Grouped product items
SizePriceStock Qty
2mg
$147.00
Ship with 10-15 days
5mg
$278.00
Ship with 10-15 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

BMS-663068 is a small-molecule attachment inhibitor of HIV-1 gp120 with IC50 value of [1].
The first step of HIV-1 virus to entry host cells is the binding of the viral gp120 envelope glycopeptide to the CD4 receptor of host cell. BMS-663068 is an attachment inhibitor against specific HIV-1 isolates and targets this step. It is a phosphonooxy methyl prodrug and can be cleaved by alkaline phosphatase in the gut then releases the effective moiety BMS-626529. Compared with the progenitor attachment inhibitorBMS-488043, BMS-663068 has an improved antivirus spectrum [1].
BMS-663068 showed low cytotoxicity in cell culture. In PM1 and PBMC cells, the CC50 values were 105 and 192 μM, respectively. In HEK293, HepG2, HCT116, HeLa, MT-2, MCF-7 and H292 cells, the CC50 values were all higher than 200 μM. It was found that BMS-663068 has potent anti-virus activity against both the laboratory strains and the clinical isolates of HIV. For the CXCR4-tropic LAI virus, BMS-663068 showed EC50 value of 0.7 nM. For a cohort of laboratory strains including NL4-3, SF-162 and JRFL, the inhibition efficacies of BMS-663068 against them were 7 to 10-fold higher than that of BMS-488043. It was even more potent than BMS-488043 when treated with 89.6 viruses (15-fold), Bal virus (14-fold) and MN virus (67-fold). In an antiviral assay using PBMC cells, BMS-663068 was treated against a total of 88 HIV-1 viruses obtained from the NIH AIDS Repository. It exerted an EC50 value of 0.01 nM against the most susceptible virus and an EC50 value of 2μM against the least susceptible virus. In addition, it was found that the virus resistant to other HIV-1 entry inhibitors such as ENF and ibalizumab retained susceptibility to BMS-626529 [1 and 2].
References:
[1] Nowicka-Sans B, Gong YF, McAuliffe B, Dicker I, Ho HT, Zhou N, Eggers B, Lin PF, Ray N, Wind-Rotolo M, Zhu L, Majumdar A, Stock D, Lataillade M, Hanna GJ, Matiskella JD, Ueda Y, Wang T, Kadow JF, Meanwell NA, Krystal M. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507.
[2] Li Z, Zhou N, Sun Y, Ray N, Lataillade M, Hanna GJ, Krystal M. Activity of the HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068, against CD4-independent viruses and HIV-1 envelopes resistant to other entry inhibitors. Antimicrob Agents Chemother. 2013 Sep;57(9):4172-80.

Chemical Properties

StorageStore at -20°C
M.Wt583.49
Cas No.864953-29-7
FormulaC25H26N7O8P
SynonymsBMS663068;BMS 663068
SolubilitySoluble in DMSO
Chemical Name(3-(2-(4-benzoylpiperazin-1-yl)-2-oxoacetyl)-4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-1-yl)methyl dihydrogen phosphate
SDFDownload SDF
Canonical SMILESCC1=NN(C2=NC=C(OC)C3=C2N(COP(O)(O)=O)C=C3C(C(N4CCN(C(C5=CC=CC=C5)=O)CC4)=O)=O)C=N1
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

BMS-663068