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Merck
CN

SBR00037

Solithromycin

≥98% (HPLC)

别名:

2H-Oxacyclotetradecino[4,3-d]oxazole-2,6,8,14(1H,7H,9H)-tetrone, CEM-101, OP-1068

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关于此项目

经验公式（希尔记法）:
C43H65FN6O10
分子量:
845.01
UNSPSC Code:
51102829
NACRES:
NA.76
MDL number:
MFCD30207880

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SMILES string

F[C@@]1(C(=O)O[C@@H]([C@]2(OC(=O)N([C@@H]2[C@H](C(=O)[C@@H](C[C@]([C@@H]([C@H](C1=O)C)O[C@@H]5O[C@@H](C[C@@H]([C@H]5O)N(C)C)C)(OC)C)C)C)CCCC[n]3nnc(c3)c4cc(ccc4)N)C)CC)C

InChI

1S/C43H65FN6O10/c1-12-32-43(8)35(50(40(55)60-43)19-14-13-18-49-23-30(46-47-49)28-16-15-17-29(45)21-28)26(4)33(51)24(2)22-41(6,56-11)37(27(5)36(53)42(7,44)39(54)58-32)59-38-34(52)31(48(9)10)20-25(3)57-38/h15-17,21,23-27,31-32,34-35,37-38,52H,12-14,18-20,22,45H2,1-11H3/t24-,25-,26+,27+,31+,32-,34-,35-,37-,38+,41-,42+,43-/m1/s1

InChI key

IXXFZUPTQVDPPK-ZAWHAJPISA-N

assay

≥98% (HPLC)

form

powder

color

white to off-white

antibiotic activity spectrum

Gram-negative bacteria, Gram-positive bacteria

mode of action

protein synthesis | interferes

storage temp.

−20°C

Quality Level

200

General description

Solithromycin is a highly potent next-generation macrolid. the first fluoroketolid. which has potent activity against most macrolide-resistant strains. Solithromycin (CEM-101) is a novel fluoroketolide with improved antimicrobial effectiveness.

Application

Solithromycin has been shown to have potentent activity against S. pneumoniae as well as an extended spectrum of activity against CA-MRS. enterococc according to in vitro and in vivo research. Solithromycin has been used in:

  • the research on the anti-inflammatory effects of macrolides
  • the research of potency of solithromycin in comparison to other antimicrobials
  • in ithe research of the vitro activity of solithromycin against clinical N. gonorrhoeae isolates and reference strain

Biochem/physiol Actions

Mode of Action: Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. Like other ketolide. it should impair bacterial ribosomal subunit formation.

Antimicrobial spectrum: Active against bacteria like Legionella, Chlamydophila, Chlamydia, Mycoplasma, and Ureaplasma and against gonococci and other organisms that cause genitourinary tract infections

Features and Benefits

High quality antibiotic suitable for mulitple research applications

Other Notes

Inxight:Drugs
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存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000146819
0000146819

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In vitro activity of the new fluoroketolide solithromycin (CEM-101) against a large collection of clinical Neisseria gonorrhoeae isolates and international reference strains, including those with high-level antimicrobial resistance: potential treatment option for gonorrhea?
Golparian et al.
Antimicrobial Agents and Chemotherapy, 56, 2739-2742 (2012)
Antimicrobial characterisation of solithromycin (CEM-101), a novel fluoroketolide: activity against staphylococci and enterococci
International Journal of Antimicrobial Agents, 37, 39-45 (2010)
Ward Rodgers et al.
Antimicrobial agents and chemotherapy, 57(4), 1632-1637 (2013-01-16)
The continuing increase in antibiotic-resistant microorganisms is driving the search for new antibiotic targets and improved antimicrobial agents. Ketolides are semisynthetic derivatives of macrolide antibiotics, which are effective against certain resistant organisms. Solithromycin (CEM-101) is a novel fluoroketolide with improved
Yoshiki Kobayashi et al.
The Journal of pharmacology and experimental therapeutics, 345(1), 76-84 (2013-01-30)
Macrolides are reported to reduce exacerbation of chronic inflammatory respiratory disease, such as chronic obstructive pulmonary disease (COPD), and also show anti-inflammatory effects in vitro and in vivo. However the anti-inflammatory efficacies of current macrolides are relatively weak. Here we

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