Aurantiamide acetate
Based on 3 publication(s) in Google Scholar
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases.
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- Purity: 99.85%
- CAS No.: 56121-42-7
- 화학식: C27H28N2O4
- 분자량:444.52
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Aurantiamide acetate
MoreAll Cathepsin Isoforms
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Biological Activity
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cathepsin L |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 2.2.15 | CC50 |
>100 μM
Compound: MTS
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Cytotoxicity against human HepG2(2.2.15) cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 29288943] |
| N9 | IC50 |
>100 μM
Compound: 24
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Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
Antineuroinflammatory activity in mouse N9 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay
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[PMID: 28073678] |
Aurantiamide acetate inhibits cathepsin L (3.4.22.15) and cathepsin B (3.4.22.1) with IC50?of 12 μM and 49 μM, respectiveiy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 56121-42-7
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Appearance Solid
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분자량 444.52
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화학식 C27H28N2O4
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Color White to off-white
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SMILES
O=C(N[C@H](COC(C)=O)CC1=CC=CC=C1)[C@@H](NC(C2=CC=CC=C2)=O)CC3=CC=CC=C3
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Synonyms
Asperglaucide
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Structure Classification
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Initial Source
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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
Publications (3)
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Journal Impact Factor
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Most Recent
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Aging (Albany NY)
2021 Aug 3;13(15):19598-19613. PMID: 34343111
용액&용해도
DMSO : 50 mg/mL (112.48 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)
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 (5.62 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 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.
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 (276 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. K Isshiki, et al. Aurantiamide Acetate, a Selective Cathepsin Inhibitor, Produced by Aspergillus Penicilloides. Biosci Biotechnol Biochem. 2001 May;65(5):1195-7. [Content Brief]
[2]. Chi-Su Yoon, et al. Anti-neuroinflammatory Effect of Aurantiamide Acetate From the Marine Fungus Aspergillus Sp. SF-5921: Inhibition of NF-κB and MAPK Pathways in Lipopolysaccharide-Induced Mouse BV2 Microglial Cells.Int Immunopharmacol. 2014 Dec;23(2):568-74. [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 | 2.2496 mL | 11.2481 mL | 22.4962 mL | 56.2404 mL |
| 5 mM | 0.4499 mL | 2.2496 mL | 4.4992 mL | 11.2481 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2496 mL | 5.6240 mL | |
| 15 mM | 0.1500 mL | 0.7499 mL | 1.4997 mL | 3.7494 mL | |
| 20 mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.8120 mL | |
| 25 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2496 mL | |
| 30 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8747 mL | |
| 40 mM | 0.0562 mL | 0.2812 mL | 0.5624 mL | 1.4060 mL | |
| 50 mM | 0.0450 mL | 0.2250 mL | 0.4499 mL | 1.1248 mL | |
| 60 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9373 mL | |
| 80 mM | 0.0281 mL | 0.1406 mL | 0.2812 mL | 0.7030 mL | |
| 100 mM | 0.0225 mL | 0.1125 mL | 0.2250 mL | 0.5624 mL |