Troleandomycin
Based on 1 Customer Validation
Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study.
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- Pureté: 99.30%
- CAS No.: 2751-09-9
- Formule: C41H67NO15
- Masse moléculaire:813.97
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Activité biologique
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CYP3 |
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Cell Line
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Type | Value | Description | References |
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| NIH-3T3-G185 | IC50 |
68.3 μM
Compound: Troleandomycin
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
78.2 μM
Compound: Troleandomycin
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TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
| NIH-3T3-G185 | IC50 |
86.3 μM
Compound: Troleandomycin
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TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells
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[PMID: 11716514] |
Troleandomycin markedly inhibits 6β-hydroxylation of testosterone, 25- and 26-hydroxylations of 5β-cholestane-3α,7α,12α-triol and 23R-, 24R-, 24S-, and 27-hydroxylations of 5β-cholestane-3α,7α,12α,25-tetrol in both recombinant CYP3A4 and microsomes, but IC50 values for microsomes are somewhat higher than those for recombinant CYP3A4[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD female rats[1].
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Dosage:500 mg/kg.
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Administration:A single oral dose.
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Result:Markedly elevated the Cmax and AUC0-6 of simvastatin by 9.5- and 10.2-fold, respectively.
Chemical Information
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CAS No. 2751-09-9
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Appearance Solid
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Masse moléculaire 813.97
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Formule C41H67NO15
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Color White to off-white
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SMILES
O=C1[C@@]2(C[C@@H]([C@@H]([C@H]([C@@H]([C@@H](C)C(O[C@H](C)[C@H](C)[C@@](OC(C)=O)([H])[C@H]1C)=O)O[C@@]3([H])C[C@@H]([C@@H](OC(C)=O)[C@H](C)O3)OC)C)O[C@@]4([H])[C@@H]([C@H](C[C@@H](C)O4)N(C)C)OC(C)=O)C)CO2
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Synonyms
Triacetyloleandomycin
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 83.33 mg/mL (102.37 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: ≥ 2.08 mg/mL (2.56 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureté et documentation
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Fiche technique (283 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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Instruction de manipulation (2659 KB)
Références
[1]. Shingen Misaka, et al. Green tea extract affects the cytochrome P450 3A activity and pharmacokinetics of simvastatin in rats. Drug Metab Pharmacokinet. 2013;28(6):514-8. [Content Brief]
[2]. A Honda, et al. Side chain hydroxylations in bile acid biosynthesis catalyzed by CYP3A are markedly up-regulated in Cyp27-/- mice but not in cerebrotendinous xanthomatosis. J Biol Chem. 2001 Sep 14;276(37):34579-85. [Content Brief]
[3]. D J Evans, et al. Troleandomycin as an oral corticosteroid steroid sparing agent in stable asthma. Cochrane Database Syst Rev. 2001;(2):CD002987. [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 |
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| DMSO | 1 mM | 1.2285 mL | 6.1427 mL | 12.2855 mL | 30.7137 mL |
| 5 mM | 0.2457 mL | 1.2285 mL | 2.4571 mL | 6.1427 mL | |
| 10 mM | 0.1229 mL | 0.6143 mL | 1.2285 mL | 3.0714 mL | |
| 15 mM | 0.0819 mL | 0.4095 mL | 0.8190 mL | 2.0476 mL | |
| 20 mM | 0.0614 mL | 0.3071 mL | 0.6143 mL | 1.5357 mL | |
| 25 mM | 0.0491 mL | 0.2457 mL | 0.4914 mL | 1.2285 mL | |
| 30 mM | 0.0410 mL | 0.2048 mL | 0.4095 mL | 1.0238 mL | |
| 40 mM | 0.0307 mL | 0.1536 mL | 0.3071 mL | 0.7678 mL | |
| 50 mM | 0.0246 mL | 0.1229 mL | 0.2457 mL | 0.6143 mL | |
| 60 mM | 0.0205 mL | 0.1024 mL | 0.2048 mL | 0.5119 mL | |
| 80 mM | 0.0154 mL | 0.0768 mL | 0.1536 mL | 0.3839 mL | |
| 100 mM | 0.0123 mL | 0.0614 mL | 0.1229 mL | 0.3071 mL |
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