Art. -Nr.: HY-109040

Quilseconazole

(Synonyms: VT-1129)

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Quilseconazole (VT-1129) is an orally active, highly selective fungal cytochrome P450 enzyme Cyp51 inhibitor that can cross the blood-brain barrier. Quilseconazole prevents the synthesis of ergosterol, an important component of the fungal cell membrane, by inhibiting Cyp51. Quilseconazole has minimal effects on human CYP enzymes. Quilseconazole has antifungal activity and can be used in the study of cryptococcal meningitis and other diseases.

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Reinheit: 98.61%
CAS. Nr.: 1340593-70-5
Formel: C₂₂H₁₄F₇N₅O₂
Molecular Weight:513.37

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Quilseconazole Chemical Structure

CAS. Nr.: 1340593-70-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CYP51

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	IC₅₀	79 μM Compound: 7c	Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method	[PMID: 24948565]

In Vitro

Quilseconazole exhibits potent antifungal activity against Cryptococcus neoformans and Cryptococcus gattii^[1].

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

In Vivo

VT-1129 (0.15-30 mg/kg; oral gavage; 10-14 days) shows antifungal activity in a mouse model of cryptococcal meningitis^[2].
Pharmacokinetic Analysis inMale CD-1 Mice^[2]

Route	Dose (mg/kg)	Plasma C_max	Brain C_max	Plasma AUC_0-96	Brain AUC_0-96
p.o.	10	3.33 μg/mL	5.24 μg/g	252 μg·h/mL	360 μg·h/g
p.o.	100	30.8 μg/mL	42.7 μg/g	2602 μg·h/mL	3231 μg·h/g

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

Animal Model:

Male ICR mice (25 g) with intracranial inoculation of Cryptococcus neoformans^[2]
Dosage:

Loading doses of 1, 3, 30 mg/kg and maintenance doses of 0.15, 0.5, 5 mg/kg
Administration:

Oral gavage; single loading dose on day 1, daily maintenance doses from day 2; treatment for 10 or 14 days
Result:

Significantly improved survival (median survival time 30 days vs. 12 days in placebo).
Reduced brain fungal burdens, and plasma/brain concentrations correlated with fungal burden reduction (R²=0.72 and 0.67, respectively).

Chemical Information

CAS. Nr. 1340593-70-5
Appearance Solid
Molecular Weight 513.37
Formel C₂₂H₁₄F₇N₅O₂
Color White to off-white
SMILES

O[C@@](CN1C=NN=N1)(C(C=CC(F)=C2)=C2F)C(F)(C3=CC=C(C4=CC=C(OC(F)(F)F)C=C4)C=N3)F
Synonyms

VT-1129
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (194.79 mM; Need ultrasonic; 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

1.9479 mL

9.7396 mL

19.4791 mL

5 mM

0.3896 mL

1.9479 mL

3.8958 mL

10 mM

0.1948 mL

0.9740 mL

1.9479 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

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]. Lockhart SR, et al. The Investigational Fungal Cyp51 Inhibitor VT-1129 Demonstrates Potent In Vitro Activity against Cryptococcus neoformans and Cryptococcus gattii. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2528-31. [Content Brief]

[2]. Wiederhold NP, et al. In Vivo Efficacy of VT-1129 against Experimental Cryptococcal Meningitis with the Use of a Loading Dose-Maintenance Dose Administration Strategy. Antimicrob Agents Chemother. 2018 Oct 24;62(11):e01315-18. [Content Brief]

[3]. Warrilow AG, et al. The Investigational Drug VT-1129 Is a Highly Potent Inhibitor of Cryptococcus Species CYP51 but Only Weakly Inhibits the Human Enzyme. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4530-8. [Content Brief]

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9479 mL	9.7396 mL	19.4791 mL	48.6978 mL
	5 mM	0.3896 mL	1.9479 mL	3.8958 mL	9.7396 mL
	10 mM	0.1948 mL	0.9740 mL	1.9479 mL	4.8698 mL
	15 mM	0.1299 mL	0.6493 mL	1.2986 mL	3.2465 mL
	20 mM	0.0974 mL	0.4870 mL	0.9740 mL	2.4349 mL
	25 mM	0.0779 mL	0.3896 mL	0.7792 mL	1.9479 mL
	30 mM	0.0649 mL	0.3247 mL	0.6493 mL	1.6233 mL
	40 mM	0.0487 mL	0.2435 mL	0.4870 mL	1.2174 mL
	50 mM	0.0390 mL	0.1948 mL	0.3896 mL	0.9740 mL
	60 mM	0.0325 mL	0.1623 mL	0.3247 mL	0.8116 mL
	80 mM	0.0243 mL	0.1217 mL	0.2435 mL	0.6087 mL
	100 mM	0.0195 mL	0.0974 mL	0.1948 mL	0.4870 mL

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Quilseconazole

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Antifungal Compound Library

Orally Active Compound Library

Mitochondria-Targeted Compound Library

Human Metabolite Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Quilseconazole

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Oxygen Sensing Compound Library

Antifungal Compound Library

Orally Active Compound Library

Mitochondria-Targeted Compound Library

Human Metabolite Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Quilseconazole Related Classifications

HY-109040 Related Classifications