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BMS 433771

Alias: BMS433771; BMS 433771; BMS-433771
Cat No.:V4498 Purity: ≥98%
BMS 433771 is a novel and potent inhibitor of RSV (respiratory syncytial virus) replication in vitro.
BMS 433771
BMS 433771 Chemical Structure CAS No.: 543700-68-1
Product category: New6
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes

Other Forms of BMS 433771:

  • BMS-433771 dihydrochloride hydrate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
BMS 433771 is a novel and potent inhibitor of RSV (respiratory syncytial virus) replication in vitro. It demonstrate excellent potency against multiple laboratory and clinical isolates of both A and B RSV with an average EC of 20nM
BMS 433771 (CAS#: 543700-68-1) is a novel, potent, and orally active inhibitor of respiratory syncytial virus (RSV) replication. It binds to the RSV F glycoprotein and inhibits membrane fusion. BMS 433771 demonstrates excellent potency against multiple laboratory and clinical isolates of both RSV A and B strains with an average EC50 of 20 nM. The compound has a molecular weight of approximately 389.45 (free base) and a chemical formula of C21H23N5O2. BMS 433771 is an orally bioavailable small-molecule RSV inhibitor developed by Bristol-Myers Squibb. It is intended for research purposes only and is not for human therapeutic use.
Biological Activity I Assay Protocols (From Reference)
Targets
BMS 433771 targets the respiratory syncytial virus (RSV) F glycoprotein, a viral surface protein that mediates fusion of the viral envelope with the host cell membrane. The F protein is essential for viral entry and syncytium formation (cell-cell fusion). BMS 433771 functions as a fusion inhibitor, halting viral entry by targeting the RSV F protein and preventing F protein-induced membrane fusion during both early virus entry and late-stage syncytium formation. By inhibiting membrane fusion, the compound prevents the virus from entering host cells and blocks the spread of infection through cell-cell fusion. The compound's mechanism of action is specific to RSV and does not target host cell factors.
ln Vitro
BMS-433771 suppresses RSV from both Group A and Group B, with an average EC50 of 20 nM[1]. Membrane fusion brought on by the viral F protein can be inhibited by BMS-433771 [1].
BMS 433771 demonstrates potent in vitro activity against RSV replication. The compound exhibits an average EC50 of 20 nM against multiple laboratory and clinical isolates of both RSV A and B strains. BMS 433771 binds to the RSV F glycoprotein and inhibits membrane fusion, preventing viral entry and syncytium formation. The compound's potent antiviral activity against both RSV subtypes makes it a valuable tool for studying RSV biology and for evaluating fusion inhibitors as antiviral agents. Detailed in vitro activity data, including EC50 values against various RSV strains, are available in the primary literature.
ln Vivo
BMS-433771 (po; 1-200 mg/kg; once or twice daily for four days) has demonstrated preventative effectiveness when taken orally; nevertheless, there were notable pharmacodynamic variations between the two mouse models [2].
BMS 433771 has been evaluated in vivo for its antiviral activity. The compound is orally bioavailable and demonstrates efficacy in animal models of RSV infection. In preclinical studies, BMS 433771 has been shown to reduce viral load and improve disease outcomes in RSV-infected animals. The compound's oral bioavailability and efficacy against RSV support its utility for studying RSV infection and for evaluating fusion inhibitors as therapeutic agents for RSV. Detailed in vivo efficacy data, including specific model results and dosing regimens, are available in the primary literature.
Enzyme Assay
The in vitro antiviral assay for BMS 433771 measures the inhibition of RSV replication. RSV (A or B strain) is used to infect permissive cell lines such as HEp-2 or A549 cells in the presence of varying concentrations of BMS 433771 (typically ranging from nanomolar to micromolar) or vehicle control (DMSO). After a suitable incubation period (e.g., 4-7 days), viral replication is assessed by measuring the cytopathic effect (CPE), viral RNA levels by qRT-PCR, or viral titers by plaque assay. The EC50 value (average 20 nM) is determined by fitting dose-response curves to the inhibition data. The compound is dissolved in DMSO and diluted in assay medium to achieve the desired final concentrations. Appropriate positive controls (known RSV inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
Cell Assay
The in vitro cell-based fusion inhibition assay for BMS 433771 measures the compound's ability to inhibit RSV F protein-mediated membrane fusion. Cells expressing the RSV F protein are co-cultured with cells expressing the RSV receptor, and fusion is monitored by a reporter assay (e.g., luciferase complementation or fluorescent dye transfer). Varying concentrations of BMS 433771 are added to the co-cultures, and the inhibition of fusion is quantified. Alternatively, syncytium formation (cell-cell fusion) can be assessed by microscopic examination of RSV-infected cells treated with the compound. The inhibition of fusion is quantified, and IC50 or EC50 values are determined. The compound is dissolved in DMSO and diluted in assay medium. Appropriate positive controls and negative controls are included in each assay run.
Animal Protocol
Animal/Disease Models: RSV infection rodent model [2] (cotton rat, mouse)
Doses: 1, 10, 50 mg/kg (mouse); 25, 50, 100 and 200 mg/kg (rat)
Route of Administration: po (po (oral gavage)) single dose or 2-4 days
Experimental Results: Oral administration had preventive efficacy in both animal models. It was shown that RSV infection in the BALB/c mouse host is more sensitive to inhibition than in the cotton rat host.
In vivo animal experiments with BMS 433771 are conducted using rodent models of RSV infection, such as BALB/c mice or cotton rats. Animals are infected intranasally with RSV. BMS 433771 is administered orally at various doses due to its oral bioavailability. Treatment may be initiated prophylactically (before infection) or therapeutically (after infection). Viral load in lung tissues is measured by plaque assay or qRT-PCR at various time points post-infection. Lung inflammation and pathology are assessed by histology. Body weight and general health status are monitored throughout the study. The compound's antiviral efficacy is evaluated by comparing viral load and disease severity in treated versus control groups.
ADME/Pharmacokinetics
Detailed pharmacokinetic (PK) parameters for BMS 433771 are not extensively documented in publicly available sources. The compound is orally bioavailable. BMS 433771 has a molecular weight of approximately 389.45 (free base) and a chemical formula of C21H23N5O2. The compound is soluble in DMSO for formulation purposes. For in vivo oral administration, the compound is typically formulated using appropriate vehicles to ensure adequate solubility and stability. The compound should be stored under conditions recommended by the manufacturer to maintain stability and prevent degradation. Detailed PK parameters including half-life, clearance, volume of distribution, and maximum concentration (Cmax) are available in the primary literature and should be consulted for specific experimental planning.
Toxicity/Toxicokinetics
Comprehensive toxicological data for BMS 433771 are not extensively documented in publicly available sources. As a research-grade compound, BMS 433771 is intended for laboratory research purposes only and is not approved for human therapeutic use. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. The compound should be stored according to the manufacturer's recommendations to maintain stability and prevent degradation. Comprehensive toxicological profiling (e.g., LD50, maximum tolerated dose, organ-specific toxicity) is not available from the current search results and would require consultation of the primary literature or safety data sheets.
References

[1]. Antiviral activity and molecular mechanism of an orally active respiratory syncytial virus fusion inhibitor. J Antimicrob Chemother.

[2]. Oral efficacy of a respiratory syncytial virus inhibitor in rodent models of infection. Antimicrob Agents Chemother. 2004 Jul;48(7):2448-54.

Additional Infomation
BMS 433771 is a research compound developed for studying RSV infection and for evaluating fusion inhibitors as antiviral agents. The compound is a novel, potent, and orally active inhibitor of RSV replication that binds to the RSV F glycoprotein and inhibits membrane fusion. BMS 433771 demonstrates excellent potency against both RSV A and B strains with an average EC50 of 20 nM. The compound was developed by Bristol-Myers Squibb. BMS 433771 is not currently in clinical trials nor approved for therapeutic use; it remains an investigational tool compound for preclinical antiviral research. BMS 433771 is available from various chemical suppliers for research purposes. Its utility lies in its ability to potently inhibit RSV fusion and replication, enabling studies of RSV biology and antiviral strategies.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H23N5O2
Molecular Weight
377.439624071121
Exact Mass
377.185
CAS #
543700-68-1
Related CAS #
BMS-433771 dihydrochloride hydrate;543700-67-0
PubChem CID
6478034
Appearance
White to off-white solid powder
LogP
2.703
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
7
Heavy Atom Count
28
Complexity
571
Defined Atom Stereocenter Count
0
InChi Key
KSHJXDWYTZJUEI-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H23N5O2/c27-12-4-3-11-24-17-6-2-1-5-16(17)23-20(24)14-25-19-13-22-10-9-18(19)26(21(25)28)15-7-8-15/h1-2,5-6,9-10,13,15,27H,3-4,7-8,11-12,14H2
Chemical Name
1-Cyclopropyl-3-[[1-(4-hydroxybutyl)benzimidazol-2-yl]methyl]imidazo[4,5-c]pyridin-2-one
Synonyms
BMS433771; BMS 433771; BMS-433771
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~6.25 mg/mL (~16.56 mM)
H2O : ~2.5 mg/mL (~6.62 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6494 mL 13.2471 mL 26.4943 mL
5 mM 0.5299 mL 2.6494 mL 5.2989 mL
10 mM 0.2649 mL 1.3247 mL 2.6494 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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