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JOSAMYCIN

Catalog No. T7148 CAS 16846-24-5

Synonyms: EN-141

Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.

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JOSAMYCIN, CAS 16846-24-5

Pack Size	Availability	Price/USD
25 mg	In stock	$ 43.00
50 mg	In stock	$ 68.00
100 mg	In stock	$ 117.00
500 mg	In stock	$ 283.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.47%

Purity: 91.38%

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Description	Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.
Targets&IC50	Ribosome:5.5 nM (Kd)
In vitro	Josamycin significantly attenuated NO production elicited by P. intermedia LPS as well as induction of iNOS protein and mRNA in RAW264.7 cells. While the release of IL-1β from cells stimulated by LPS was suppressed in the presence of josamycin, josamycin failed to reduce the degree of IL-1β mRNA expression. Josamycin did not reduce the stability of IL-1β mRNA induced by P. intermedia LPS, at the same time josamycin also failed to suppress the LPS-induced intracellular IL-1β expression. Josamycin augmented HO-1 induction in cells exposed to P. intermedia LPS, and SnPP, an inhibitor of HO-1 activity, reversed the suppressive impact of josamycin upon NO generation induced by LPS. Josamycin diminished NF-κB transcriptional activity induced by P. intermedia LPS. Further, josamycin enhanced SOCS1 mRNA level in cells activated with LPS[1].
In vivo	Josamycin (0.1%) was topically administered to NC/Nga mice with AD-like skin lesions induced by 2, 4, 6-trinitrochlorobenzene (TNCB). The therapeutic effects of josamycin were assessed by measurement of the skin severity scores, histological changes in the lesioned skin, serum levels of total IgE, and expression of interferon (IFN)-γ and interleukin (IL)-4 in lymph nodes and skin lesions[2].
Cell Research	LPS was purified by employing phenol-water extraction protocol. Culture supernatants were analyzed for nitric oxide (NO) and interleukin (IL)-1β. Real-time PCR and immunoblotting were conducted to quantify mRNA and protein expression, respectively. The expression levels of IL-1β were analyzed by confocal laser scanning microscopy. NF-κB-dependent SEAP levels were estimated by reporter assay[1].
Animal Research	Topical treatment with josamycin significantly suppressed the increase in the skin severity score in NC/Nga mice. This suppressive effect was equal to that of betamethasone, and was associated with a decrease in the density of cellular infiltration into the dermis, the mast cell count in the dermis and the serum IgE level. Furthermore, topical application of josamycin reduced the expression of IFN-γ and IL-4 in auricular lymph node cells and the skin lesions[2].

Synonyms	EN-141
Molecular Weight	827.99
Formula	C42H69NO15
CAS No.	16846-24-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 41.67 mg/mL (50.33 mM)

References and Literature

1. Eun-Young C , So-Hui C , Jin-Yi H , et al. Josamycin suppresses, Prevotella intermedia, lipopolysaccharide-induced production of nitric oxide and interleukin-1β in murine macrophages[J]. Biomedicine & Pharmacotherapy, 2018, 105:498-505. 2. Katsuhiko M , Kanta T , Kei O , et al. Topical Application of Josamycin Inhibits Development of Atopic Dermatitis-Like Skin Lesions in NC/Nga Mice[J]. Journal of Pharmacy & Pharmaceutical Sciences, 2017, 20:38-. 3. Auzou M , Caillon J , Poyart C , et al. In vitro activity of josamycin against Streptococcus pyogenes isolated from patients with upper respiratory tract infections in France[J]. MÃ©decine et Maladies Infectieuses, 2015, 45(7):293-296.

Related compound libraries

This product is contained In the following compound libraries：

Microbial Natural Product Library Drug Repurposing Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Bacterial Compound Library Bioactive Compounds Library Max Anti-Tumor Natural Product Library Clinical Compound Library Natural Product Library Covalent Inhibitor Library Approved Drug Library

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Keywords

JOSAMYCIN 16846-24-5 Microbiology/Virology Antibacterial Antibiotic inhibit EN141 EN 141 Inhibitor EN-141 Bacterial inhibitor

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