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JNJ-678 (JNJ-53718678) (Synonyms: JNJ-678; JNJ-53718678)

Catalog No.GC32297

JNJ-678 (JNJ-53718678) (JNJ-678) is a novel fusion protein inhibitor.

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JNJ-678 (JNJ-53718678) Chemical Structure

Cas No.: 1383450-81-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$50.00
In stock
5mg
$45.00
In stock
10mg
$77.00
In stock
25mg
$162.00
In stock
50mg
$279.00
In stock
100mg
$486.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

The antiviral activity of JNJ-678 (JNJ-53718678) against hMPV is evaluated using a cellular infectious assay in 96-well plates in which Vero/TMPRSS2 cells are infected with recombinant hMPV65. Cells are treated with different concentrations of JNJ-678 (JNJ-53718678) and then infected with recombinant hMPV (1×104 PFU per well). Three days post-virus exposure, viral replication is quantified by measuring fluorescence and the EC50 is calculated[1].

Animal experiment:

Rats[1]Cotton rats receive either a single dose at 24 h after viral infection or once-daily doses of 40 mg/kg JNJ-678 (JNJ-53718678) by oral gavage, at 24, 48, and 72 h after viral infection. The decrease of viral replication in all experiments is compared to challenged animals that received only the vehicle[1].

References:

[1]. Roymans D, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167.

Background

JNJ-678 (JNJ-53718678) is a novel fusion protein inhibitor in clinical trials for the treatment of respiratory syncytial virus (RSV).

JNJ-678 (JNJ-53718678) is a small-molecule respiratory syncytial virus (RSV) fusion inhibitor currently under clinical evaluation in infants hospitalized for RSV infection. JNJ-678 (JNJ-53718678) binds to RSV F protein in its prefusion conformation. JNJ-678 (JNJ-53718678) displays very potent antiviral activity and low cytotoxicity. In addition to its activity against the RSV A2 strain, JNJ-678 (JNJ-53718678) is also highly active against a number of RSV strains from both A and B subtypes. The EC50 in an RSV infection assay using HeLa cells is 460 pM[1].

Oral treatment of neonatal lambs with JNJ-678 (JNJ-53718678), or with an equally active close analog, efficiently inhibits established acute lower respiratory tract infection in the animals, even when treatment is delayed until external signs of respiratory syncytial virus illness have become visible[1].

[1]. Roymans D, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167.

Chemical Properties

Cas No. 1383450-81-4 SDF
Synonyms JNJ-678; JNJ-53718678
Canonical SMILES O=C(N1CC(F)(F)F)N(CC(N2CCCS(=O)(C)=O)=CC3=C2C=CC(Cl)=C3)C4=C1C=CN=C4
Formula C21H20ClF3N4O3S M.Wt 500.92
Solubility DMSO : 65 mg/mL (129.76 mM);Water : < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9963 mL 9.9816 mL 19.9633 mL
5 mM 0.3993 mL 1.9963 mL 3.9927 mL
10 mM 0.1996 mL 0.9982 mL 1.9963 mL
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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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Average Rating: 5 ★★★★★ (Based on Reviews and 4 reference(s) in Google Scholar.)

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