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Art. -Nr.: HY-12930

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SPR719

(Synonyms: VXc-486)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

SPR719 (VXc-486) is an orally active gyrase B inhibitor, with bactericidal activity. SPR719 potently inhibits multiple agent-sensitive isolates and drug-resistant isolates of Mycobacterium tuberculosis, with MICs of 0.03 to 0.30 μg/ml and 0.08 to 5.48 μg/ml, respectively. SPR719 is promising for research of lung disease caused by non-tuberculous mycobacteria (NTM).

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Reinheit: 99.39%
CAS. Nr.: 1384984-18-2
Formel: C₂₁H₂₅FN₆O₃
Molecular Weight:428.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SPR719 Chemical Structure

CAS. Nr.: 1384984-18-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

gyrase B^[1]

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

In Vitro

SPR719 inhibits M. tuberculosis replication in macrophages with a MIC range of 0.125-0.25 μg/mL^[1]^[2].

IC₅₀ (μg/ml) of SPR719 for indicated isolate in macrophages^[1]

Compound	H37Ra	CDC1551
SPR719	0.012	0.115

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

In Vivo

SPR719 (100 mg/kg, oral gavage, twice a day for 4 weeks) combined with pVXc-486 (30 and 100 mg/kg, oral gavage, twice a day for 4 weeks) reduces the mycobacterial burden in a model of chronic tuberculosis infection in mice^[1].

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

Animal Model:

Chronic tuberculosis mouse model^[1]
Dosage:

100 mg/kg
Administration:

oral gavage, twice a day for 4 weeks
Result:

Significantly reduced the median mycobacterial lung burdens in a chronic tuberculosis mouse model.

Chemical Information

CAS. Nr. 1384984-18-2
Appearance Solid
Molecular Weight 428.46
Formel C₂₁H₂₅FN₆O₃
Color Yellow to brown
SMILES

O=C(NC1=NC2=CC(C3=CN=C(C(C)(O)C)N=C3)=C(F)C([C@@H]4OCCC4)=C2N1)NCC
Synonyms

VXc-486
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Cell

Genome-wide gene expression tuning reveals diverse vulnerabilities of M. tuberculosis. [Abstract]

2021 Aug 19;184(17):4579-4592.e24. PMID: 34297925
ACS Infect Dis

Role of DNA Double-Strand Break Formation in Gyrase Inhibitor-Mediated Killing of Nonreplicating Persistent Mycobacterium tuberculosis in Caseum. [Abstract]

2024 Oct 11;10(10):3631-3639. PMID: 39315541
Antimicrob Agents Chemother

Activity of Oral Tebipenem-Avibactam in a Mouse Model of Mycobacterium abscessus Lung Infection. [Abstract]

2023 Feb 16;67(2):e0145922. PMID: 36688684
Antimicrob Agents Chemother

Piperidine-4-Carboxamides Target DNA Gyrase in Mycobacterium abscessus. [Abstract]

2021 Jul 16;65(8):e0067621. PMID: 34001512

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 20 mg/mL (46.68 mM; ultrasonic and adjust pH to 2 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3339 mL

11.6697 mL

23.3394 mL

5 mM

0.4668 mL

2.3339 mL

4.6679 mL

10 mM

0.2334 mL

1.1670 mL

2.3339 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Locher CP, et al. A novel inhibitor of gyrase B is a potent drug candidate for treatment of tuberculosis and nontuberculosis mycobacterial infections. Antimicrob Agents Chemother. 2015 Mar;59(3):1455-65. [Content Brief]

[2]. Pidot SJ, et al. In vitro activity of SPR719 against Mycobacterium ulcerans, Mycobacterium marinum and Mycobacterium chimaera. PLoS Negl Trop Dis. 2021 Jul 26;15(7):e0009636. [Content Brief]

[3]. Aragaw WW, et al. In Vitro Resistance against DNA Gyrase Inhibitor SPR719 in Mycobacterium avium and Mycobacterium abscessus. Microbiol Spectr. 2022 Feb 23;10(1):e0132121. [Content Brief]

[4]. Cotroneo N, et al. In vitro activity and in vivo efficacy against non-tuberculous mycobacteria of SPR719, the active moiety of the novel oral benzimidazole prodrug SPR720[J]. bioRxiv, 2022: 2022.12. 08.519697.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3339 mL	11.6697 mL	23.3394 mL	58.3485 mL
	5 mM	0.4668 mL	2.3339 mL	4.6679 mL	11.6697 mL
	10 mM	0.2334 mL	1.1670 mL	2.3339 mL	5.8349 mL
	15 mM	0.1556 mL	0.7780 mL	1.5560 mL	3.8899 mL
	20 mM	0.1167 mL	0.5835 mL	1.1670 mL	2.9174 mL
	25 mM	0.0934 mL	0.4668 mL	0.9336 mL	2.3339 mL
	30 mM	0.0778 mL	0.3890 mL	0.7780 mL	1.9450 mL
	40 mM	0.0583 mL	0.2917 mL	0.5835 mL	1.4587 mL

Keywords

SPR719

4 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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SPR719

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SPR719

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SPR719

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) SPR719

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SPR719 Related Classifications

HY-12930 Related Classifications