Carumonam
Carumonam (AMA-1080; Ro 17-2301) is a sulfonated monocyclic β-Lactam Antibiotic, targeting to penicillin-binding protein (PBP). Carumonam exerts highly activity against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae, while it weakly and even inactively inhibits Streptococcus pneumoniae and Staphylococcus aureus. Carumonam is resistant to beta-lactamase-mediated hydrolysis.
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- CAS No.: 87638-04-8
- Formule: C12H14N6O10S2
- Masse moléculaire:466.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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β-lactam |
Carumonam shows inhibition against Enterobacteriaceae isolates with MIC90 values of 0.013-25 μg/mL, while it inhibits P. aeruginosa with a MIC90 value of 12.5 μg/mL[1].
Carumonam (0-400 μg/mL) has high affinity to binding PBP-3 in Enterobacteriaceae and P. aeruginosa with IC50s as same with or smaller than the MICs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal: Five-week-old male Slc:ICR mice (20-25 g), 7-week-old male Jcl:SD rats (210-250 g), male New Zealand White rabbits (2.5-3.5 kg), male and female beagle dogs (10-15 kg), and female cynomolgus monkeys (2.8-3.7 kg). They are deprived of feed for 16 to 18 h before the antibiotic was administered; water was given ad libitum[2].
Pharmacokinetic Analysis[2]
| Animal | Dose (mg/kg) | Route | Tmax (h) | Cmax (μg/mL) | AUC (μg·h/mL) | t1/2 (h) | CLp (mL/min/kg) |
| Mouse | 2 mg/mL, 0.1 mL/10 g | s.c. | 0.12 | 40.7 | 20.0 | 0.24 | 16.7 |
| Rat | 10 mg/mL, 0.2 mL/100 g | i.m. | 0.18 | 37.9 | 23.9 | 0.28 | 14.0 |
| Rabbit | 40 mg/mL, 0.5 mL/kg | i.m. | 0.36 | 44.9 | 66.6 | 0.73 | 5.0 |
| Dog | 100 mg/mL, 0.2 mL/kg | i.m. | 0.36 | 36.3 | 61.1 | 1.10 | 5.5 |
| Monkey | 20 mg/mL/kg | i.m. | 0.29 | 67.9 | 80.4 | 0.89 | 4.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 87638-04-8
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Masse moléculaire 466.40
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Formule C12H14N6O10S2
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SMILES
O=C(CO/N=C(C(N[C@H]1[C@H](N(C1=O)S(=O)(O)=O)COC(N)=O)=O)/C2=CSC(N)=N2)O
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Synonyms
AMA-1080; Ro 17-2301
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Imada A, et al. In vitro and in vivo antibacterial activities of carumonam (AMA-1080), a new N-sulfonated monocyclic beta-lactam antibiotic. Antimicrob Agents Chemother. 1985 May;27(5):821-7. [Content Brief]
[2]. Kita Y, et al. Comparative pharmacokinetics of carumonam and aztreonam in mice, rats, rabbits, dogs, and cynomolgus monkeys. Antimicrob Agents Chemother. 1986 Jan;29(1):127-34. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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