Name | doripenem hydrate |
Synonyms | DoripeneM Crude doripenem hydrate S 4661 monohydrate (4R,5S,6S)-6-((R)-1-Hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((sulfamoylamino)methyl)pyrroli (4R,5S,6S)-6-[(1R)-1-Hydroxyethyl]-4-methyl-7-oxo-3-[(3S,5S)-5-[(sulfamoylamino)methyl]pyrrolidin-3-yl]sulfanyl-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid, 3-[[(3S,5S)-5-[[(aminosulfonyl)amino]methyl]-3-pyrrolidinyl]thio]-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-, hydrate (+)-(4r,5s,6s)-6-[(1r)-1-hydroxyethyl]-4-methyl-7-oxo-3-[[(3s,5s)-5-[(sulfamoylamino)-methyl]-3-pyrrolidinyl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate |
CAS | 364622-82-2 |
EINECS | 680-392-3 |
InChI | InChI=1/C15H24N4O6S2.H2O/c1-6-11-10(7(2)20)14(21)19(11)12(15(22)23)13(6)26-9-3-8(17-5-9)4-18-27(16,24)25;/h6-11,17-18,20H,3-5H2,1-2H3,(H,22,23)(H2,16,24,25);1H2/t6-,7-,8+,9+,10-,11-;/m1./s1 |
InChIKey | NTUBEBXBDGKBTJ-WGLOMNHJSA-N |
Molecular Formula | C15H26N4O7S2 |
Molar Mass | 438.51 |
Melting Point | 173°C(dec.)(lit.) |
Boling Point | 694.8°C at 760 mmHg |
Flash Point | 374°C |
Solubility | H2O: soluble5mg/mL, clear (warmed) |
Vapor Presure | 2.49E-22mmHg at 25°C |
Appearance | powder |
Color | white to beige |
BRN | 15340136 |
PH | Dissolve 0.3g of Doripenem Hydrate in 30mL of water: the pH of the solution is between 4.5 and 6.0. |
Storage Condition | 2-8°C |
In vitro study | Doripenem is effective against Aeromonas(MIC50 is 0.03 mg/L),Bacillus spp.(MIC50,0.03 mg/L) and all anaerobic species tested (MIC range 0.015-4 mg/L), but against S. maltophilia(MIC 90> 32 mg/L) and Enterococcus faecium(MIC90 >32 mg/L) were not highly active. Doripenem was the most active carbapenem with a MIC 90 of 1 to 4 mg/mL against penicillin-resistant streptococci. Doripenem has high activity against oxacillin-sensitive Staphylococcus aureus and coagulase-negative Staphylococcus aureus (2705 and 297 strains, MIC90s up to 0.06 mg/L), potency is greater than other carbapenem antibiotics. Doripenem is one of the most effective drugs tested against Streptococcus pneumoniae, Streptococcus viridans group Streptococcus and β-hemolytic Streptococcus (885,140 and 397 isolates; MIC(90) 0.5, respectively, 0.5 and 0.03 mg/L). Doripenem is also very active against Citrobacter, Enterobacter, and Salmonella (MIC90s 0.06-0.25 mg/L), including ceftazidime-resistant strains. Doripenem is more effective (MIC50 is 2 mg/L) than ertapenem and imipenem(MIC50 is 4 mg/L), and against Burkholderia cepacia (20 strains) it has a potency similar to that of meropenem (MIC50 is 2 mg/L). Doripenem has activity similar to meropenem against gram-negative pathogens, and in vitro activity similar to imipenem against gram-positive pathogens. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.28 ml | 11.402 ml | 22.804 ml |
5 mM | 0.456 ml | 2.28 ml | 4.561 ml |
10 mM | 0.228 ml | 1.14 ml | 2.28 ml |
5 mM | 0.046 ml | 0.228 ml | 0.456 ml |