Home Immunology & Inflammation gp120/CD4 inhibitor Fostemsavir For research use only.

Fostemsavir

Synonyms: BMS-663068, Rukobia

Fostemsavir (BMS-663068, Rukobia), the phosphonooxymethyl prodrug of BMS626529, is an attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells with EC50 of < 10 nM.

Fostemsavir Chemical Structure

Fostemsavir Chemical Structure

CAS: 864953-29-7

Purity & Quality Control

Batch: S722001 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.65%
99.65

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Biological Activity

Description Fostemsavir (BMS-663068, Rukobia), the phosphonooxymethyl prodrug of BMS626529, is an attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells with EC50 of < 10 nM.
Targets
HIV-1 gp120 [1]
(Cell-free assay)
10 nM(EC50)
In Vivo
In vivo

BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529 designed to increase the solubility of the compound in the gut. BMS-663068 is cleaved by alkaline phosphatase, located on the luminal surface of the small intestine brush border membranes, releasing BMS-626529. Due to its good membrane permeability, BMS-626529 is then rapidly absorbed.[1] BMS-663068 is an orally active inhibitor of HIV-1 attachment.[2]
Animal Research Animal Models C57BL/7 mice, NSG-SGM3-derived HSC-Hu mice
Dosages 20 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04648280 Recruiting HIV Infections With Multi Drug Resistant Virus PENTA Foundation|ViiV Healthcare|PHPT Foundation|Hospital Universitario 12 de Octubre|Cromsource June 30 2022 Phase 1|Phase 2
NCT05220358 Recruiting HIV-1-infection Orlando Immunology Center|ViiV Healthcare May 1 2022 Phase 4
NCT02805556 Completed Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline March 15 2016 Phase 1
NCT02508064 Completed Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline August 3 2015 Phase 1
NCT02362503 Active not recruiting HIV Infections ViiV Healthcare February 23 2015 Phase 3

Chemical lnformation & Solubility

Molecular Weight 583.49 Formula

C25H26N7O8P
CAS No. 864953-29-7 SDF --
Smiles COC1=CN=C([N]2C=NC(=N2)C)C3=C1C(=C[N]3CO[P](O)(O)=O)C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (171.38 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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