[CAS NO. 87638-04-8] Carumonam
PRODUCTS SPECIFICATIONS [87638-04-8]
DESCRIPTION [87638-04-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 466.40 |
| Molecular Formula | C12H14N6O10S2 |
| 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 |
Summary
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 [1] .
IC50 & Target
Penicillin-binding protein, PBP [1]
In Vitro
Carumonam shows inhibition against
Enterobacteriaceae
isolates with MIC
90
values of 0.013-25 μg/mL, while it inhibits
P. aeruginosa
with a MIC
90
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 IC
50
s as same with or smaller than the MICs
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Carumonam (20 mg/kg; s.c. or i.m.; single dose) is easily absorbed and distributes in high concentrations in plasma, kidneys, liver and lungs in pharmacokinetic analysis in mice, rats, rabbits, dogs and cynomolgus monkeys
[2]
.
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 | T max (h) | C max (μg/mL) | AUC (μg·h/mL) | t 1/2 (h) | CL p (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 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [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.
- [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.