Antrafenine
Based on 1 Customer Validation
Antrafenine (Stakane) is a derivative of 2-(quinolin-4-ylamino) benzoate, and is an orally active anti-inflammatory and analgesic agent. Antrafenine protects mammalian epithelial cells from cell death upon exposure to influenza A virus A/WSN/33 (H1N1). Antrafenine inhibits carrageenan-induced paw swelling in rats, and reduces exudate volume and total leukocyte infiltration in carrageenan- and calcium pyrophosphate dihydrate crystal-induced pleurisy in rats. Antrafenine can be used in studies related to influenza and pseudogout.
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- Purity : 99.76%
- CAS No.: 55300-29-3
- 화학식: C30H26F6N4O2
- 분자량:588.54
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MDCK | CC50 |
>100 μM
Compound: 38
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Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
Cytotoxicity against MDCK cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
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[PMID: 37672932] |
In Vitro
Antrafenine (compound 38) (100 μM; 24 hours-2 days) shows weak cytopathic protection but minimal virus inhibitory activity against influenza A/WSN/33 (H1N1) in MDCK cells, with no significant inhibition observed at 100 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Antrafenine (10-40 mg/kg; p.o.; single dose) suppresses carrageenan-induced pleurisy in male CD Sprague Dawley rats, with an ED40 of 15 mg/kg p.o. for exudate volume reduction and 33 mg/kg p.o. for leucocyte infiltration reduction[2].
Antrafenine (10-40 mg/kg; p.o.; single dose) suppresses calcium pyrophosphate dihydrate crystal-induced pleurisy in male CD Sprague Dawley rats, with an ED40 of 20 mg/kg p.o. for exudate volume reduction and 40 mg/kg p.o. for leucocyte infiltration reduction[2].
Antrafenine (200-400 mg/kg; p.o.; single dose) exhibits mild acute ulcerogenic activity in fasted male CD Sprague Dawley rats at oral doses of 200 and 400 mg/kg, with mean ulcer scores of 0.58 and 0.65 respectively and no mortality[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD Sprague Dawley (male, 160-180 g, carrageenan-induced paw oedema model)[2]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:p.o.; single dose
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Result:Suppressed paw oedema volume by 15%, 34%, 55% at 10, 20, 40 mg/kg, with an oral ED40 of 24 mg/kg.
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Animal Model:CD Sprague Dawley (male, 160-180 g, carrageenan-induced pleurisy model)[2]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:p.o.; single dose
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Result:Suppressed exudate volume by 33%, 44%, 60% at 10, 20, 40 mg/kg, with an oral ED40 of 15 mg/kg.
Suppressed total leucocytes by 27%, 36%, 42% at 10, 20, 40 mg/kg, with an oral ED40 of 33 mg/kg for infiltration inhibition.
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Animal Model:CD Sprague Dawley (male, 160-180 g, calcium pyrophosphate dihydrate crystal-induced pleurisy model)[2]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:p.o.; single dose
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Result:Decreased exudate volume by 33%, 37%, 50% at 10, 20, 40 mg/kg respectively.
Possessed an oral ED40 of 20 mg/kg for exudate suppression.
Decreased total leucocytes by 25%, 31%, 39% at 10, 20, 40 mg/kg respectively.
Possessed an oral ED40 of 40 mg/kg for leucocyte infiltration suppression.
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Animal Model:CD Sprague Dawley (male, 160-180 g, fasted acute ulcerogenicity model)[2]
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Dosage:200 mg/kg; 400 mg/kg
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Administration:p.o.; single dose
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Result:Yielded mean ulcer scores of 0.58 (200 mg/kg, comparable to controls) and 0.65 (400 mg/kg, distinct from controls).
Triggered zero mortality at both doses.
Chemical Information
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CAS No. 55300-29-3
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Appearance Solid
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분자량 588.54
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화학식 C30H26F6N4O2
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Color White to off-white
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SMILES
O=C(OCCN1CCN(C2=CC=CC(C(F)(F)F)=C2)CC1)C3=CC=CC=C3NC4=CC=NC5=CC(C(F)(F)F)=CC=C45
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Synonyms
Stakane
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (169.91 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. 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. 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.25 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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.
순도&문서
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Tang YS, et al. Anti-influenza virus activities and mechanism of antrafenine analogs. Eur J Med Chem. 2023 Nov 15;260:115775. [Content Brief]
[2]. Dunn CJ, et al. Antrafenine: anti-inflammatory activity with respect to oedema and leucocyte infiltration in the rat. Agents Actions. 1984 Feb;14(2):296-9. [Content Brief]
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. 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 | 1.6991 mL | 8.4956 mL | 16.9912 mL | 42.4780 mL |
| 5 mM | 0.3398 mL | 1.6991 mL | 3.3982 mL | 8.4956 mL | |
| 10 mM | 0.1699 mL | 0.8496 mL | 1.6991 mL | 4.2478 mL | |
| 15 mM | 0.1133 mL | 0.5664 mL | 1.1327 mL | 2.8319 mL | |
| 20 mM | 0.0850 mL | 0.4248 mL | 0.8496 mL | 2.1239 mL | |
| 25 mM | 0.0680 mL | 0.3398 mL | 0.6796 mL | 1.6991 mL | |
| 30 mM | 0.0566 mL | 0.2832 mL | 0.5664 mL | 1.4159 mL | |
| 40 mM | 0.0425 mL | 0.2124 mL | 0.4248 mL | 1.0619 mL | |
| 50 mM | 0.0340 mL | 0.1699 mL | 0.3398 mL | 0.8496 mL | |
| 60 mM | 0.0283 mL | 0.1416 mL | 0.2832 mL | 0.7080 mL | |
| 80 mM | 0.0212 mL | 0.1062 mL | 0.2124 mL | 0.5310 mL | |
| 100 mM | 0.0170 mL | 0.0850 mL | 0.1699 mL | 0.4248 mL |
Antrafenine Related Classifications
HY-A0235 Related Classifications
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Keywords
- Antrafenine
- 55300-29-3
- Stakane
- Drug Derivative
- Influenza Virus
- calcium pyrophosphate dihydrate crystal-induced pleurisies
- leucocyte infiltration
- carrageenan-induced paw oedema
- pseudogout
- influenza virus A/WSN/33 (H1N1)
- rats
- influenza
- mammalian epithelial cells
- male CD Sprague Dawley rats
- MDCK cells
- Inhibitor
- inhibitor
- inhibit