Saperconazole (Synonyms: R66905)

Cat. No.: HY-U00249 Purity: 99.35%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Saperconazole (R66905) is a broad-spectrum antifungal triazole and has potent activity against Aspergillus with an MIC₉₀ of 0.19 mg/L.

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

Saperconazole Chemical Structure

CAS No. : 110588-57-3

Size	Price	Stock	Quantity
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1100	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1700	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

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

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Saperconazole (R66905) is a broad-spectrum antifungal triazole and has potent activity against Aspergillus with an MIC₉₀ of 0.19 mg/L.

IC₅₀ & Target

MIC90: 0.19 mg/L^[1]

In Vitro

The antifungal activity of Saperconazole is complete at 1 μg/mL for all but one strain of A. niger. Eighty percent of all strains show complete absence of growth at 0.1 μg/mL (85% for A. fumigatus), and this result persists during 14 days of the test^[2].

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

In Vivo

All control pigeons infect with A. fumigatus die within 2 to 5 days. They have necrotic foci in the lungs, air sacs, liver, spleen, and kidneys. These organs are highly positive by histology and oncultures. Saperconazole administered at 2.5 mg/kg is not active, but when it is given at 5 or 10 mg/kg, 92 or 100%, respectively, survive and organ cultures are negative. No drug-related side effects are observed in the pigeons^[2].

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

Molecular Weight

672.72

Formula

C₃₅H₃₈F₂N₈O₄

CAS No.

110588-57-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1N(C(C)CC)N=CN1C2=CC=C(N3CCN(C4=CC=C(OCC5OC(CN6N=CN=C6)(C7=CC=C(F)C=C7F)OC5)C=C4)CC3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (37.16 mM; ultrasonic and warming and heat to 60°C; 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	1.4865 mL	7.4325 mL	14.8650 mL
5 mM	0.2973 mL	1.4865 mL	2.9730 mL
10 mM	0.1487 mL	0.7433 mL	1.4865 mL

View the Complete Stock Solution Preparation Table

* 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.72 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)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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

Purity: 99.35%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (248 KB) HNMR (276 KB) RP-HPLC (255 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. [Content Brief]

[2]. VVan Cutsem J, et al. Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals. Antimicrob Agents Chemother. 1989 Dec;33(12):2063-8. [Content Brief]

Cell Assay ^[2]	A total of 279 Aspergillus isolates are tested in vitro; 221 of these are A. fumigatus. The inoculum consists of a standardized 4 mm² culture block containing hyphae and spores for tubes with 5 mL of medium supplemented with drug solution or with solvent^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Male immunocompetent (normal) or immunocompromised pigs weighing 500 g (±50 g) are infected intravenously (i.v.) with 25,000 CFU of A.fumigatus B19119 per g of body weight. The animals are treated orally with Saperconazole, ketoconazole, or fluconazole dissolved in polyethylene glycol 200 (PEG 200). The treatment is given once daily for 14 consecutive days, starting on the day of infection or on day 1, 2, 3, or 4 after infection. Saperconazole, dissolved in dimethyl-β-cyclodextrin and in hydroxypropyl-β-cyclodextrin is also administered i.p. and i.v. Pigeons with a mean weight of 400 g (±30 g) are infected i.v. in a wing vein with 7,800 CFU of A.fumigatus B19119 per g of body weight. Saperconazole dissolved in PEG 200 is administered by gavage at 0, 2.5, 5, or 10 mg/kg starting on the day of infection and continued once daily for 14 consecutive days^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Otcenásek M, et al. Susceptibility of clinical isolates of fungi to saperconazole. Mycopathologia. 1992 Jun;118(3):179-83. [Content Brief] [2]. VVan Cutsem J, et al. Oral and parenteral therapy with saperconazole (R 66905) of invasive aspergillosis in normal and immunocompromised animals. Antimicrob Agents Chemother. 1989 Dec;33(12):2063-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.4865 mL	7.4325 mL	14.8650 mL	37.1626 mL
	5 mM	0.2973 mL	1.4865 mL	2.9730 mL	7.4325 mL
	10 mM	0.1487 mL	0.7433 mL	1.4865 mL	3.7163 mL
	15 mM	0.0991 mL	0.4955 mL	0.9910 mL	2.4775 mL
	20 mM	0.0743 mL	0.3716 mL	0.7433 mL	1.8581 mL
	25 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4865 mL
	30 mM	0.0496 mL	0.2478 mL	0.4955 mL	1.2388 mL

Saperconazole 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:

Saperconazole110588-57-3R66905R 66905R-66905FungalInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks