2. Anti-infection Metabolic Enzyme/Protease
  3. Fungal Cytochrome P450
  4. Quilseconazole

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.

For research use only. We do not sell to patients.

Quilseconazole Chemical Structure

Quilseconazole Chemical Structure

CAS No. : 1340593-70-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Quilseconazole:

Quilseconazole Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target

CYP51

 

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.

Quilseconazole Related Antibodies
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 Cmax Brain Cmax Plasma AUC0-96 Brain AUC0-96
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).
Molecular Weight

513.37

Formula

C22H14F7N5O2
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9479 mL 9.7396 mL 19.4791 mL
5 mM 0.3896 mL 1.9479 mL 3.8958 mL
View the Complete Stock Solution Preparation Table

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • 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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Quilseconazole Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Quilseconazole1340593-70-5VT-1129VT1129VT 1129FungalCytochrome P450CYPsCryptococcus neoformansCryptococcus gattiicryptococcal meningitis modelInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Quilseconazole
Cat. No.:
HY-109040
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

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) Portuguese - PT (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.