| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Purity: ≥98%
| ln Vitro |
The 6β-structuring of testosterone, the 25- and 26-unionization of 5β-cholestane-3α, 7α, and 12α-triol, and the 23R-, 24R-, and 24S of 5β-cholestane-3α, 7α are all markedly inhibited by troleandomycin. microsomes include 12- and 27-recombinant, recombinant CYP3A4 as well as 12α, 25-tetraol; nevertheless, microsomes' IC50 value is marginally greater than recombinant CYP3A4's [1].
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|---|---|
| ln Vivo |
In both mouse and human liver cancer, troleandomycin mimic substantially reduces microsomal side chain anchoring [2].
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| Animal Protocol |
Animal/Disease Models: SD female rat[1].
Doses: 500 mg/kg. Doses: Single oral dose. Experimental Results: The Cmax and AUC0-6 of simvastatin were Dramatically increased by 9.5 times and 10.2 times respectively. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Troleandomycin has known human metabolites that include [(3R,5S,6S,7R,8S,9R,12R,13S,14S,15R)-8-[(2R,4S,5S,6S)-5-acetyloxy-4-methoxy-6-methyloxan-2-yl]oxy-6-[(2S,3R,4S,6R)-3-acetyloxy-6-methyl-4-(methylamino)oxan-2-yl]oxy-5,7,9,12,13,15-hexamethyl-10,16-dioxo-1,11-dioxaspiro[2.13]hexadecan-14-yl] acetate. |
| References |
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| Additional Infomation |
Troleandomycin is a semi-synthetic macrolide antibiotic obtained by acetylation of the three free hydroxy groups of oleandomycin. Troleandomycin is only found in individuals that have taken the drug. It has a role as an EC 1.14.13.97 (taurochenodeoxycholate 6alpha-hydroxylase) inhibitor and a xenobiotic. It is a macrolide antibiotic, a polyketide, a monosaccharide derivative, an epoxide, an acetate ester and a semisynthetic derivative. It is functionally related to an oleandomycin.
A macrolide antibiotic that is similar to erythromycin. A macrolide antibiotic that is similar to ERYTHROMYCIN. Drug Indication For the treatment of bacterial infection. Mechanism of Action As a macrolide, troleandomycin binds to the 50S subunit of the bacterial ribosome. This binding inhibits translocation of tRNA along the A, P, and E sites of the ribosome. With tRNA unable to move from site to site, amino acids cannot be deposited onto the polypeptide chain leading to failure of protein synthesis. Bacterial cell growth and duplication is inhibited without the ability to generate the necessary proteins. Pharmacodynamics Troleandomycin, like other macrolide antibiotics, inhibits bacterial protein synthesis to prevent growth. |
| Molecular Formula |
C41H67NO15
|
|---|---|
| Molecular Weight |
813.968380000001
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| Exact Mass |
813.451
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| CAS # |
2751-09-9
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| PubChem CID |
202225
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| Appearance |
White to off-white solid powder
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| Density |
1.19g/cm3
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| Boiling Point |
812.5ºC at 760mmHg
|
| Melting Point |
170 °C (lit.)
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| Flash Point |
445.2ºC
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| Vapour Pressure |
1.82E-26mmHg at 25°C
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| Index of Refraction |
1.515
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| LogP |
3.62
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
57
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| Complexity |
1430
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| Defined Atom Stereocenter Count |
18
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| SMILES |
C[C@@H]1C[C@@H]([C@H]([C@@H](O1)O[C@H]2[C@H](C[C@@]3(CO3)C(=O)[C@@H]([C@H]([C@H]([C@H](OC(=O)[C@@H]([C@H]([C@@H]2C)O[C@H]4C[C@@H]([C@H]([C@@H](O4)C)OC(=O)C)OC)C)C)C)OC(=O)C)C)C)OC(=O)C)N(C)C
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| InChi Key |
LQCLVBQBTUVCEQ-QTFUVMRISA-N
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| InChi Code |
InChI=1S/C41H67NO15/c1-19-17-41(18-49-41)38(46)23(5)34(53-27(9)43)21(3)25(7)52-39(47)24(6)35(56-32-16-31(48-14)36(26(8)51-32)54-28(10)44)22(4)33(19)57-40-37(55-29(11)45)30(42(12)13)15-20(2)50-40/h19-26,30-37,40H,15-18H2,1-14H3/t19-,20+,21-,22+,23+,24+,25+,26-,30-,31-,32-,33-,34-,35-,36-,37+,40-,41+/m0/s1
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| Chemical Name |
[(3R,5S,6S,7R,8S,9R,12R,13S,14S,15R)-6-[(2S,3R,4S,6R)-3-acetyloxy-4-(dimethylamino)-6-methyloxan-2-yl]oxy-8-[(2R,4S,5S,6S)-5-acetyloxy-4-methoxy-6-methyloxan-2-yl]oxy-5,7,9,12,13,15-hexamethyl-10,16-dioxo-1,11-dioxaspiro[2.13]hexadecan-14-yl] acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~102.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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