Fostemsavir

For research use only.

Catalog No.S7220 Synonyms: BMS-663068, Rukobia

Fostemsavir Chemical Structure

CAS No. 864953-29-7

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.

Purity & Quality Control

Choose Selective gp120/CD4 Inhibitors

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

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]

Protocol

Animal Research:

[2]

- Collapse
  • Animal Models: C57BL/7 mice, NSG-SGM3-derived HSC-Hu mice
  • Dosages: 20 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (171.38 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 583.49
Formula

C25H26N7O8P

CAS No. 864953-29-7
Storage powder
in solvent
Synonyms BMS-663068, Rukobia

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04648280 Not yet recruiting Drug: Fostemsavir HIV Infections With Multi Drug Resistant Virus PENTA Foundation|ViiV Healthcare|PHPT Foundation|Hospital Universitario 12 de Octubre|Cromsource June 2021 Phase 1|Phase 2
NCT02805556 Completed Drug: BMS-663068|Drug: BMS-626529 Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline March 15 2016 Phase 1
NCT02508064 Completed Drug: BMS-663068 Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline August 3 2015 Phase 1
NCT02362503 Active not recruiting Drug: BMS-663068|Other: Placebo HIV Infections ViiV Healthcare February 23 2015 Phase 3
NCT02467335 Completed Drug: BMS-663068 Infection Human Immunodeficiency Virus ViiV Healthcare|GlaxoSmithKline January 29 2015 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Related gp120/CD4 Products

Tags: buy Fostemsavir | Fostemsavir supplier | purchase Fostemsavir | Fostemsavir cost | Fostemsavir manufacturer | order Fostemsavir | Fostemsavir distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID