- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: Josamycin
- Price:
- Purity: 98.0%
- Stocking Period: 10 Day
- Contact: Yang
- Shanghai Jizhi Biochemical Technology Co., Ltd
- China
- Product Name: Josamycin
- Price: ￥3628.0/10mg
- Purity: 98.0%
- Stocking Period: 1 Day
- Contact: Liu jia
- DC Chemicals Limited
- China
- Product Name: Josamycin
- Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/500mg
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
- ShangHai DC Chemicals Co.,Ltd
- China
- Product Name: Josamycin
- Price: ￥Inquiry/1g
- Purity: 98.9%
- Stocking Period: 1 Day
- Contact: Tony Lai
- Henan Tianfu Chemical Co., Ltd.
- China
- Product Name: JOSAMYCIN(16846-24-5)
- Price: $Inquiry/1kg $Inquiry/25kg $Inquiry/1000kg $Inquiry/10ton
- Purity: 99.0%
- Stocking Period: Inquiry
- Contact: Anson
16846-24-5
16846-24-5 structure
- Name: Josamycin
- Chemical Name: josamycin
- CAS Number: 16846-24-5
- Molecular Formula: C42H69NO15
- Molecular Weight: 827.995
- Catalog: API Antibiotics Macrolide drug
- Create Date: 2018-02-12 08:00:00
- Modify Date: 2024-01-02 14:42:19
-
Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.
| Name | josamycin |
|---|---|
| Synonyms |
(2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-Acetoxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate
Iosalide 4-(acetyloxy)-6-((3,6-dideoxy-4-O-(2,6-dideoxy-3-C-methyl-4-O-(3-methyl-1-oxobutyl)-α-L-ribo-hexopyranosyl)-3-(dimethylamino)-β-D-glucopyranosyl)oxy)-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxooxacyclohexadeca-11,13-diene-7-acetaldehyde Vilprafen Leucomycin V 3-Acetate 4B-(3-Methylbutanoate) MFCD00211043 Leucomycin A3 EN 141 Josamina EINECS 240-871-6 JOSAMYCIN carbomycin B Jomybel (2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-(acetyloxy)-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate (non-preferred name) YL-704A3 Wilprafen Josacine (2S,3R,4R,6S)-6-{[(2R,3S,4R,5R,6S)-6-{[(4R,6S,7R,9R,10R,11E,13E,16R)-4-Acetoxy-10-hydroxy-5-methoxy-9,16-dimethyl-2-oxo-7-(2-oxoethyl)oxacyclohexadeca-11,13-dien-6-yl]oxy}-4-(dimethylamino)-5-hydroxy-2-methyltetrahydro-2H-pyran-3-yl]oxy}-4-hydroxy-2,4-dimethyltetrahydro-2H-pyran-3-yl 3-methylbutanoate (non-preferred name) |
| Description | Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity against a wide spectrum of pathogens, such as bacteria. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM. |
|---|---|
| Related Catalog | |
| Target |
Kd: 5.5 nM (ribosome)[1] |
| In Vitro | Studies show that the average lifetime on the ribosome is 3 h for Josamycin and that the dissociation constants for Josamycin binding to the ribosome is 5.5 nM. Josamycin slows down formation of the first peptide bond of a nascent peptide in an amino acid-dependent way and completely inhibits formation of the second or third peptide bond, depending on peptide sequence at a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin. At a saturating drug concentration, synthesis of fulllength proteins is completely shut down by Josamycin[1]. |
| In Vivo | Blood and tissue levels of Josamycin after oral administration are 200 mg/kg to rabbits. Tissue levels are generally much higher than the blood levels, and 3 h after the administration, when the blood level is very low, the tissue levels are rather higher than those 1 h after the dose. One hour after the medication, the level in the lungs is the highest of all the tissue levels[2]. |
| Kinase Assay | Josamycin is prepared in polymix buffer, containing 5 mM magnesium acetate, 5 mM ammonium chloride, 95 mM potassium chloride, 0.5 mM calcium chloride, 8 mM putrescine, 1 mM spermidine, 5 mM potassium phosphate, and 1 mM dithioerythritol. Josamycin at different concentrations (2, 3, 4, and 6 μM is added to preinitiated ribosomes to start the incubation. One volume of elongation mix is added to 1 volume of reaction mix at each incubation time, and after 10 s the reaction is quenched with formic acid. The association rates are estimated from the fraction of tri-peptide-forming ribosomes[1]. |
| Animal Admin | Rat: Tritium-labelled Josamycin (200 mg/kg) is orally administrated to rats. The blood and tissue levels are determined at 1 h and 3 h by bioassay[2]. Mouse: Tritium-labelled Josamycin (200 mg/kg) is orally administrated to mice. The blood and tissue levels are determined at 1 h and 3 h by bioassay[2]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 877.8±65.0 °C at 760 mmHg |
| Melting Point | 131.5℃ |
| Molecular Formula | C42H69NO15 |
| Molecular Weight | 827.995 |
| Flash Point | 484.7±34.3 °C |
| Exact Mass | 827.466736 |
| PSA | 206.05000 |
| LogP | 3.88 |
| Vapour Pressure | 0.0±0.6 mmHg at 25°C |
| Index of Refraction | 1.535 |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
|
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
| WGK Germany | 2 |
| RTECS | OH4725810 |