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Art. -Nr.: HY-184048

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JMX0207

JMX0207 is an orally active flavivirus NS2B-NS3 protease inhibitor. JMX0207 showed an IC_50-SLC of 1.3 μM for blocking NS2B-NS3 protein interaction and an IC_50-pro of 8.2 μM for inhibiting protease catalytic activity.. JMX0207 directly binds viral NS3 protease at the NS2B-NS3 interface with a K_d of 1.1 μM, blocks viral polyprotein precursor processing, suppresses viral RNA replication and viral protein production. JMX0207 can be used for the study of Zika virus infection and Dengue virus infection.

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CAS. Nr.: 33580-97-1
Formel: C₁₃H₈ClN₃O₆
Molecular Weight:337.67

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

JMX0207 Chemical Structure

CAS. Nr.: 33580-97-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

DENV2 NS3 protease

1.1 μM (Kd)

In Vitro

JMX0207 inhibits the molecular interaction between viral NS3 and its cofactor NS2B in the split luciferase complementation assay, with an IC_50-SLC of 1.3 μM^[1].
JMX0207 inhibits DENV2 NS2B-NS3 activity with an IC_50-pro of 8.2 μM^[1].
JMX0207 directly binds viral NS3 protease with a K_d of 1.1 μM in the SPR assay, and protein thermal shift assay shows that JMX0207 binding stabilizes viral NS3 protease with a 0.75 ℃ increase in T_m^[1].
JMX0207 (0.01-10 μM; 48 h) inhibits DENV2 infectivity in A549 cells with an EC_50-DN2 of 0.31 μM, and shows a CC₅₀ of 31.9 μM^[1].
JMX0207 (0.19-5 μM) reduces ZIKV RNA copy number and viral E antigen production in ZIKV-infected A549 cells in a dose-dependent manner, with an EC_50-ZK of 0.30 μM^[1].
JMX0207 (0.03-7.5 μM) reduces ZIKV viral protein expression and viral RNA synthesis in human neural progenitor cells (HNPCs) in a dose-dependent manner^[1].
JMX0207 (1.5 μM) protects iPSC-derived 3D mini-brain organoids from ZIKV infection and reduces ZIKV production^[1].
JMX0207 (0.75 μM; 0-24 h) remains effective when added up to 24 h postinfection, indicating that JMX0207 inhibits viral replication rather than viral entry^[1].
JMX0207 inhibits DENV2 replication in a DENV2 replicon cell line with an EC_50-DN2 of 1.1 μM^[1].
JMX0207 (0.19-0.75 μM; 48 h postinfection) reduces ZIKV NS3 protein production and increases high-molecular-weight unprocessed viral polyprotein precursor in ZIKV-infected A549 cells in a dose-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[1]

Cell Line:

A549
Concentration:

0.19, 0.38, 0.75, 1.5, 5 μM
Incubation Time:

48 h postinfection
Result:

Reduced ZIKV RNA copy number in a dose-dependent manner in ZIKV-infected A549 cells.

Immunofluorescence^[1]

Cell Line:

A549
Concentration:

0.19, 0.56, 1.67, 5 μM
Incubation Time:

48 h postinfection
Result:

Reduced ZIKV viral E protein production in a dose-dependent manner, as shown by pan-flavivirus anti-E 4G2 antibody staining.

Western Blot Analysis^[1]

Cell Line:

A549
Concentration:

0.19, 0.38, 0.75 μM
Incubation Time:

48 h postinfection
Result:

Reduced ZIKV NS3 protein production in a dose-dependent manner.
Increased accumulation of high-molecular-weight unprocessed viral polyprotein precursor recognized by anti-ZIKV NS3 antibody.
Supported inhibition of viral protease function and viral polyprotein precursor processing.

Immunofluorescence^[1]

Cell Line:

iPSC-derived 3D mini-brain organoids
Concentration:

1.5 μM
Incubation Time:

5 dpi for PFU assay; 7 dpi for fluorescence imaging
Result:

Showed no obvious toxic effect on 3D organoids and maintained organoid morphology.
Nearly completely protected 3D mini-brain organoids from ZIKV infection.
Reduced ZIKV antigen production across organoid layers and significantly decreased ZIKV production from the organoids.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	AUC_0-∞
Mice^[1]	40 mg/kg	p.o.	1.2 h	145 μM	11 h	2719 μM/L·h

In Vivo

JMX0207 (20 mg/kg/day; p.o.; once daily; for 3 days postinfection) significantly reduces ZIKV-induced viremia in A129 mice inoculated with PRVABC59 ZIKV^[1].
JMX0207 (40 mg/kg/day; p.o.; once daily; for 7 days) shows no signs of toxicity in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Four-week-old A129 mice inoculated with 1.7 × 10⁵ PFU PRVABC59 ZIKV^[1]
Dosage:

20 mg/kg/day
Administration:

Oral gavage (p.o.); once daily; for 3 days postinfection
Result:

Significantly reduced ZIKV-induced viremia compared with vehicle control.
Viremia was measured by plaque forming unit (PFU) assay on day 3 postinfection.
Showed in vivo antiviral activity against ZIKV after oral administration.

Animal Model:

Adult female B6 mice ^[1]
Dosage:

40 mg/kg/day
Administration:

Oral gavage (p.o.); once daily; for 7 days
Result:

Displayed no sign of toxicity during repeated oral dosing.
Supported low toxicity and acceptable in vivo tolerability at 40 mg/kg/day.

Chemical Information

CAS. Nr. 33580-97-1
Molecular Weight 337.67
Formel C₁₃H₈ClN₃O₆
SMILES

O=C(C1=CC=CC([N+]([O-])=O)=C1O)NC2=CC=C([N+]([O-])=O)C=C2Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li Z et al. JMX0207, a Niclosamide Derivative with Improved Pharmacokinetics, Suppresses Zika Virus Infection Both In Vitro and In Vivo. ACS Infect Dis. 2020 Oct 9;6(10):2616-2628. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

MOQ

Minimum order quantity

100 mg

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