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Chemical Structure| 120410-24-4 Chemical Structure| 120410-24-4

Structure of Biapenem
CAS No.: 120410-24-4

Chemical Structure| 120410-24-4

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Biapenem, belonging to pentacyclic triterpenoids, exhibits antimicrobial activity against reference strains of methicillin-resistant and methicillin-sensitive S. aureus.

Synonyms: CLI 86815; L 627; Omegacin

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Product Details of Biapenem

CAS No. :120410-24-4
Formula : C15H18N4O4S
M.W : 350.39
SMILES Code : O=C1[C@H]([C@H](O)C)[C@@]2([H])[C@@H](C)C(SC(C3)CN4[N+]3=CN=C4)=C(C([O-])=O)N12
Synonyms :
CLI 86815; L 627; Omegacin
MDL No. :MFCD00864863
InChI Key :MRMBZHPJVKCOMA-YJFSRANCSA-N
Pubchem ID :71339

Safety of Biapenem

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse peritoneal macrophages 10 μg/mL 48 h To assess the effect of BPM on ROS levels in macrophages, results showed that BPM significantly increases ROS levels, and this effect was reversed by the antioxidant NAC. Microbiol Spectr. 2023 Aug 17;11(4):e0085823
mice peritoneal macrophages 10 μg/mL 48 h To evaluate the inhibitory effect of BPM on the intracellular growth of M.tb in macrophages, results showed that BPM significantly enhances the ability of macrophages to restrict M.tb growth. Microbiol Spectr. 2023 Aug 17;11(4):e0085823
Bacteroides spp. 0.5 to 16 μg/ml Biapenem-RPX7009 showed activity comparable to that of imipenem and was superior to meropenem, doripenem, and ertapenem against imipenem-nonsusceptible Bacteroides spp. Antimicrob Agents Chemother. 2013 Jun;57(6):2620-30
Anaerobic bacteria 0.03 to 32 μg/ml Biapenem alone and in combination with RPX7009 showed excellent activity that was comparable to that of meropenem. Antimicrob Agents Chemother. 2013 Jun;57(6):2620-30
Veillonella parvula 0.06 μg/ml 48 h To test the in vitro activity of Biapenem against Veillonella parvula, the results showed MIC at 0.06 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Peptostreptococcus spp. 0.12-2 μg/ml 48 h To test the in vitro activity of Biapenem against Peptostreptococcus spp., the results showed MIC range of 0.12-2 μg/ml, with MIC for 90% of strains at 2 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Clostridium spp. 0.12-1 μg/ml 48 h To test the in vitro activity of Biapenem against Clostridium spp., the results showed MIC range of 0.12-1 μg/ml, with MIC for 90% of strains at 1 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Eubacterium spp. 0.12-0.5 μg/ml 48 h To test the in vitro activity of Biapenem against Eubacterium spp., the results showed MIC range of 0.12-0.5 μg/ml, with MIC for 90% of strains at 0.12 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Prevotella disiens 0.06-0.12 μg/ml 48 h To test the in vitro activity of Biapenem against Prevotella disiens, the results showed MIC range of 0.06-0.12 μg/ml, with MIC for 90% of strains at 0.12 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Prevotella bivia 0.12 μg/ml 48 h To test the in vitro activity of Biapenem against Prevotella bivia, the results showed MIC at 0.12 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Bacteroides capillosus 0.06-0.12 μg/ml 48 h To test the in vitro activity of Biapenem against Bacteroides capillosus, the results showed MIC range of 0.06-0.12 μg/ml, with MIC for 90% of strains at 0.12 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Bacteroides fragilis group 0.12-2 μg/ml 48 h To test the in vitro activity of Biapenem against Bacteroides fragilis group, the results showed MIC range of 0.12-2 μg/ml, with MIC for 90% of strains at 0.25 μg/ml. Antimicrob Agents Chemother. 1994 Apr;38(4):889-93
Bacteroides fragilis 0.25-1 μg/ml 48 h Biapenem inhibited all strains of B. fragilis at concentrations of ≤1 μg/ml Antimicrob Agents Chemother. 1993 Sep;37(9):2009-16
Pseudomonas aeruginosa 0.25-4 μg/ml 20 h Biapenem was active against Pseudomonas aeruginosa (MIC90 = 1 μg/ml) Antimicrob Agents Chemother. 1993 Sep;37(9):2009-16
Escherichia coli 0.06-8 μg/ml 20 h Biapenem was active against Escherichia coli (MIC90 = 0.25 μg/ml) Antimicrob Agents Chemother. 1993 Sep;37(9):2009-16
Staphylococcus aureus (Methicillin-susceptible strains) 0.06-0.125 μg/ml 20 h Biapenem was active against methicillin-susceptible Staphylococcus aureus (MIC90 = 0.125 μg/ml) Antimicrob Agents Chemother. 1993 Sep;37(9):2009-16
Pseudomonas aeruginosa KMX7803 32 μg/ml 3 h To compare the tolerance of mutant and wild-type to biapenem, the mutant exhibited significantly higher survival rates. Antimicrob Agents Chemother. 2003 Sep;47(9):2997-3001
Mycobacterium tuberculosis 124R 8–16 mg/L 14 days To evaluate the antimicrobial activity of Biapenem alone and in combination with rifampicin against the high-level rifampicin-resistant strain 124R, results showed that Biapenem alone was active against 124R but did not exhibit synergy with rifampicin (FICI 1.0). J Antimicrob Chemother. 2017 Aug 1;72(8):2320-2325
Mycobacterium tuberculosis 115R 4–8 mg/L 14 days To evaluate the antimicrobial activity of Biapenem alone and in combination with rifampicin against the low-level rifampicin-resistant strain 115R, results showed that Biapenem alone was active against 115R and exhibited synergy with rifampicin (FICI 0.15). J Antimicrob Chemother. 2017 Aug 1;72(8):2320-2325
Mycobacterium tuberculosis H37Rv 2–4 mg/L 14 days To evaluate the antimicrobial activity of Biapenem alone and in combination with rifampicin against H37Rv, results showed that Biapenem alone was active against H37Rv and exhibited synergy with rifampicin (FICI 0.28). J Antimicrob Chemother. 2017 Aug 1;72(8):2320-2325

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Low dose aerosol infection with M.tb H37Rv Intraperitoneal 5 mg/kg Thrice a week for 60 days To evaluate the inhibitory effect of BPM on M.tb growth in vivo, results showed that BPM significantly reduces bacterial load in the lungs and spleen of infected mice. Microbiol Spectr. 2023 Aug 17;11(4):e0085823

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01702649 Healthy Volunteers ... More >> Bacterial Infections Less << Phase 1 Completed - United States, Arizona ... More >> Celerion Tempe, Arizona, United States, 85283 Less <<
NCT01772836 Healthy Volunteers ... More >> Bacterial Infections Less << Phase 1 Completed - Australia, South Australia ... More >> CMAX Adelaide, South Australia, Australia, 5000 Less <<
NCT01751269 Healthy Volunteers ... More >> Bacterial Infections Less << Phase 1 Completed - Australia, South Australia ... More >> CMAX Adelaide, South Australia, Australia, 5000 Less <<
NCT04552444 High-dose Biapenem UNKNOWN 2021-08-01 The Second Affiliated Hospital... More >> of Zhejiang University Medical College, Hangzhou, Please Select, 310000, China Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.54mL

5.71mL

2.85mL

References

 

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