Antifungal agent 136
Based on 1 Customer Validation
Antifungal agent 136 is a CYP51 inhibitor and antifungal agent. Antifungal agent 136 downregulates the expression of interleukin-6 to alleviate inflammatory responses. Antifungal agent 136 exhibits activity against both drug-sensitive and drug-resistant Candida albicans strains. Antifungal agent 136 can be used in the research of fungal infections and inflammatory diseases.
For research use only. We do not sell to patients.
- Purity: 99.15%
- CAS No.: 3075607-57-4
- Formula: C20H22F2N4OS2
- Molecular Weight:436.54
-
Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Anti-Infection Compound Library
HY-L002
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Aging Compound Library
HY-L034
-
Antioxidant Compound Library
HY-L037
-
Differentiation Inducing Compound Library
HY-L038
-
Oxygen Sensing Compound Library
HY-L045
-
Antifungal Compound Library
HY-L048
-
Angiogenesis-Related Compound Library
HY-L088
-
Mitochondria-Targeted Compound Library
HY-L089
-
Metabolic Enzyme Compound Library
HY-L146
-
Highly Selective Inhibitors Library
HY-L158
-
Cytokine Inhibitors Library
HY-L161
-
Anti-Drug-Resistant Compound Library
HY-L169
-
Multi-Target Compound Library
HY-L176
-
Radioprotector Library
HY-L178
-
MCE Bioactive Compound Library
HY-L001V
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
|
CYP51 |
Antifungal agent 136 (M-15) (0.002 μg/mL) exhibited an MIC80 of 0.002 μg/mL against sensitive Candida albicans SC5314, which was 250 times more active than Fluconazole (HY-B0101)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Antifungal agent 136 (1mg/kg; i.p.; daily; 3 consecutive days) exhibits superior antifungal activity to Fluconazole (HY-B0101) and Voriconazole (HY-76200) in a mouse model of drug-resistant systemic candidiasis, as measured by reduced kidney fungal load and no treatment-related deaths[1].
Antifungal agent 136 (1mg/kg; i.p.; daily; 3 consecutive days) significantly downregulates kidney IL-6 mRNA expression in immunocompetent mice with systemic candidiasis, reducing inflammation far more effectively than voriconazole[1].
Antifungal agent 136 (1mg/kg; i.p.; daily; 3 consecutive days) significantly downregulates kidney IL-6 mRNA expression in immunosuppressed mice with systemic candidiasis, reducing inflammation more effectively than voriconazole[1].
Antifungal agent 136 (1mg/kg; i.p.; daily; 3 consecutive days) significantly downregulates kidney IL-6 mRNA expression in severely immunosuppressed mice with systemic Candida infection, reducing inflammation far more effectively than voriconazole (HY-76200)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:unspecified (immunosuppressed via cyclophosphamide 100mg/kg i.p.)[1]
-
Dosage:1mg/kg
-
Administration:i.p.; daily; 3 consecutive days
-
Result:Prevented all animal deaths.
Reduced kidney fungal load (log10 CFU/g) to a level lower than that of the fluconazole group.
Demonstrated superior antifungal activity compared to fluconazole.\nPrevented all animal deaths.
Reduced kidney fungal load (log10 CFU/g) to a level lower than that of the fluconazole and voriconazole groups.
Demonstrated superior antifungal activity compared to both control drugs.
-
Animal Model:unspecified (immunocompetent)[1]
-
Dosage:1mg/kg
-
Administration:i.p.; daily; 3 consecutive days
-
Result:Significantly reduced kidney IL-6 mRNA expression by dozens of-fold compared to voriconazole.
In contrast, voriconazole treatment increased IL-6 mRNA to over 300-fold relative to baseline, while post-infection baseline IL-6 mRNA expression reached nearly 200-fold relative to pre-infection levels.
-
Animal Model:unspecified (immunosuppressed via cyclophosphamide 50mg/kg i.p.)[1]
-
Dosage:1mg/kg
-
Administration:i.p.; daily; 3 consecutive days
-
Result:Significantly reduced kidney IL-6 mRNA expression compared to voriconazole.
Post-infection baseline IL-6 mRNA expression reached nearly 350-fold relative to pre-infection levels, while voriconazole treatment increased IL-6 mRNA to over 200-fold relative to baseline.
-
Animal Model:unspecified (severely immunosuppressed via cyclophosphamide 100mg/kg i.p.)[1]
-
Dosage:1mg/kg
-
Administration:i.p.; daily; 3 consecutive days
-
Result:Significantly reduced kidney IL-6 mRNA expression compared to voriconazole.
Post-infection baseline IL-6 mRNA expression reached nearly 800-fold relative to pre-infection levels, while voriconazole treatment increased IL-6 mRNA to over 700-fold relative to baseline.
Chemical Information
-
CAS No. 3075607-57-4
-
Appearance Solid-Liquid Mixture
-
Molecular Weight 436.54
-
Formula C20H22F2N4OS2
-
Color Off-white to light yellow
-
SMILES
C[C@@H](SSCCCC1=CC=NC=C1)[C@@](O)(C2=C(C=C(C=C2)F)F)CN3C=NC=N3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (229.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.45 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.45 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal 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
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 (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (277 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)
-
Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 2.2907 mL | 11.4537 mL | 22.9074 mL | 57.2685 mL |
| 5 mM | 0.4581 mL | 2.2907 mL | 4.5815 mL | 11.4537 mL | |
| 10 mM | 0.2291 mL | 1.1454 mL | 2.2907 mL | 5.7269 mL | |
| 15 mM | 0.1527 mL | 0.7636 mL | 1.5272 mL | 3.8179 mL | |
| 20 mM | 0.1145 mL | 0.5727 mL | 1.1454 mL | 2.8634 mL | |
| 25 mM | 0.0916 mL | 0.4581 mL | 0.9163 mL | 2.2907 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7636 mL | 1.9090 mL | |
| 40 mM | 0.0573 mL | 0.2863 mL | 0.5727 mL | 1.4317 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4581 mL | 1.1454 mL | |
| 60 mM | 0.0382 mL | 0.1909 mL | 0.3818 mL | 0.9545 mL | |
| 80 mM | 0.0286 mL | 0.1432 mL | 0.2863 mL | 0.7159 mL | |
| 100 mM | 0.0229 mL | 0.1145 mL | 0.2291 mL | 0.5727 mL |
Antifungal agent 136 Related Classifications
HY-W1127089 Related Classifications
Powered by Bioz