Art. -Nr.: HY-108881

Troleandomycin

(Synonyms: Triacetyloleandomycin)

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Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study.

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Reinheit: 99.30%
CAS. Nr.: 2751-09-9
Formel: C₄₁H₆₇NO₁₅
Molecular Weight:813.97

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Troleandomycin Chemical Structure

CAS. Nr.: 2751-09-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor. Troleandomycin is an oral corticosteroid for asthma study^[1]^[2]^[3].

IC₅₀ & Target

CYP3

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NIH-3T3-G185	IC₅₀	68.3 μM Compound: Troleandomycin	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	78.2 μM Compound: Troleandomycin	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	86.3 μM Compound: Troleandomycin	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]

In Vitro

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.

In Vivo

Troleandomycin markedly suppresses these microsomal side chain hydroxylations in both mouse and human livers in a dose-dependent manner^[2].

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

Animal Model:

SD female rats^[1].
Dosage:

500 mg/kg.
Administration:

A single oral dose.
Result:

Markedly elevated the C_max and AUC_0-6 of simvastatin by 9.5- and 10.2-fold, respectively.

Chemical Information

CAS. Nr. 2751-09-9
Appearance Solid
Molecular Weight 813.97
Formel C₄₁H₆₇NO₁₅
Color White to off-white
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
Synonyms

Triacetyloleandomycin
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2285 mL

6.1427 mL

12.2855 mL

5 mM

0.2457 mL

1.2285 mL

2.4571 mL

10 mM

0.1229 mL

0.6143 mL

1.2285 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (2.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	1.2285 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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Troleandomycin

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FDA Approved & Pharmacopeial Drug Library

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MCE Bioactive Compound Library

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Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Troleandomycin

Anti-Infection Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Antioxidant Compound Library

Lipid Compound Library

Oxygen Sensing Compound Library

Antibacterial Compound Library

FDA Approved & Pharmacopeial Drug Library

Antibiotics Library

Mitochondria-Targeted Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Troleandomycin Related Classifications

HY-108881 Related Classifications