| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
Biapenem (also called L-627, CLI 86815, LJC10627) is a potent carbapenem antibiotic with activity against both Gram-positive and Gram-negative bacterial strains. Biapenem has activity comparable to those of Imipenem and Meropenem against all groups of anaerobes with MICs for 90% of the strains tested of 0.06 to 2 mg/mL. Biapenem is more active than ampicillin-sulbactam, ticarcillin-clavulanate, piperacillin, cefoxitin, cefotaxime, and ceftriaxone. Biapenem is also active against all of the B. capillosus, Prevotella, Clostridium, and Eubacterium strains and anaerobic cocci tested. Biapenem shows broad antibacterial activity against both Gram-positive and Gram-negative clinical isolates.
| Targets |
β-lactam
Bacterial Penicillin-Binding Proteins (PBPs) (MIC values: Escherichia coli = 0.03-0.12 μg/mL; Klebsiella pneumoniae = 0.06-0.25 μg/mL; Staphylococcus aureus = 0.12-0.5 μg/mL) [1][2][3] |
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| ln Vitro |
Biapenem has activity comparable to those of Imipenem and Meropenem against all groups of anaerobes with MICs for 90% of the strains tested of 0.06 to 2 mg/mL. Biapenem is more active than ampicillin-sulbactam, ticarcillin-clavulanate, piperacillin, cefoxitin, cefotaxime, and ceftriaxone. Biapenem is also active against all of the B. capillosus, Prevotella, Clostridium, and Eubacterium strains and anaerobic cocci tested. Biapenem shows broad antibacterial activity against both Gram-positive and Gram-negative clinical isolates. Biapenem is found to be approximately as active as imipenem, inhibiting 90% of isolates of most species at concentrations within one dilution of the MIC of imipenem for 90% of the isolates.
Biapenem (CLI 86815) exhibits broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria. For Gram-negative bacteria: it inhibited Escherichia coli (including ESBL-producing strains) with MIC50 = 0.06 μg/mL, MIC90 = 0.12 μg/mL; Klebsiella pneumoniae with MIC50 = 0.12 μg/mL, MIC90 = 0.25 μg/mL; Pseudomonas aeruginosa with MIC50 = 1 μg/mL, MIC90 = 2 μg/mL [1][2][3] - For Gram-positive bacteria: it suppressed Staphylococcus aureus (methicillin-susceptible, MSSA) with MIC50 = 0.25 μg/mL, MIC90 = 0.5 μg/mL; Streptococcus pneumoniae with MIC50 = 0.03 μg/mL, MIC90 = 0.06 μg/mL; Enterococcus faecalis with MIC50 = 1 μg/mL, MIC90 = 2 μg/mL [1][3] - It showed bactericidal activity: time-kill curve assays demonstrated that at 2×MIC, it reduced viable counts of Escherichia coli by ≥3 log10 CFU/mL within 6 hours and Pseudomonas aeruginosa by ≥3 log10 CFU/mL within 8 hours [1][2] - It is stable to most β-lactamases (ESBLs, AmpC β-lactamases) but susceptible to metallo-β-lactamases (MBLs) [3][4] - No cytotoxicity to human epithelial cells (HEp-2) or fibroblasts (NHF) at concentrations up to 100 μg/mL [1] |
| ln Vivo |
Biapenem results in significantly fewer viable bacteria than in the lungs of control mice. Biapenem prevents the progression of lung inflammation, including alveolar neutrophil infiltration and hemorrhage. Biapenem significantly prolongs survival and reduces the number of viable bacteria in a murine model of VAP caused by P. aeruginosa.
In mice with Escherichia coli-induced intra-abdominal sepsis, intravenous administration of Biapenem (CLI 86815) (5 mg/kg, 10 mg/kg, 20 mg/kg, every 8 hours for 3 days) dose-dependently improved survival. Survival rates were 40% (5 mg/kg), 75% (10 mg/kg), and 90% (20 mg/kg), compared to 10% in the vehicle control group. It reduced bacterial load in peritoneal fluid by ~6 log10 CFU/mL at 20 mg/kg [1] - In rats with Pseudomonas aeruginosa-induced pneumonia, intratracheal administration of Biapenem (CLI 86815) (10 mg/kg, 20 mg/kg, once daily for 5 days) alleviated lung infection: lung bacterial counts decreased by ~4 log10 CFU/g (10 mg/kg) and ~5 log10 CFU/g (20 mg/kg); histological analysis showed reduced pulmonary inflammation and edema [2] - In a phase III clinical trial , intravenous Biapenem (CLI 86815) (300 mg every 8 hours for 7-14 days) achieved clinical cure rates of 85% in community-acquired pneumonia, 82% in complicated urinary tract infections, and 78% in intra-abdominal infections, comparable to meropenem [4] |
| Enzyme Assay |
Bacterial PBP binding assay: Purified PBPs (PBP1a, PBP2, PBP3) from Escherichia coli were incubated with Biapenem (CLI 86815) (0.01-10 μg/mL) and radiolabeled penicillin G at 37°C for 30 minutes. SDS-PAGE electrophoresis and autoradiography were performed to quantify PBP binding inhibition, confirming high affinity for PBP2 and PBP3 [1]
- MIC determination assay: Bacteria were inoculated into Mueller-Hinton broth containing serial dilutions of Biapenem (CLI 86815) (0.001-128 μg/mL) and incubated at 37°C for 18-24 hours. The lowest concentration inhibiting visible bacterial growth was defined as MIC [1][2][3] - β-lactamase stability assay: Biapenem (CLI 86815) (10 μg/mL) was incubated with purified β-lactamases (ESBLs, AmpC, MBLs) at 37°C for 1 hour. Residual antibacterial activity was measured by agar diffusion assay, with inhibition zone diameter used to evaluate stability [3] |
| Cell Assay |
Time-kill curve assay: Bacterial suspensions (10⁶ CFU/mL) were incubated with Biapenem (CLI 86815) at 0.5×MIC, 1×MIC, 2×MIC, and 4×MIC at 37°C. Aliquots were sampled at 0, 2, 4, 6, 8, and 24 hours, serially diluted, and plated on agar plates. Colonies were counted after 24 hours to determine viable bacterial counts [1][2]
- Cytotoxicity assay: Human HEp-2 cells and NHF cells were seeded in 96-well plates and treated with Biapenem (CLI 86815) (0.1-100 μg/mL) for 24 hours. MTT reagent was added, and absorbance at 570 nm was measured to evaluate cell viability [1] |
| Animal Protocol |
Mouse intra-abdominal sepsis model: CD-1 mice were intraperitoneally inoculated with Escherichia coli (10⁸ CFU/mouse) mixed with 5% mucin. Biapenem (CLI 86815) was dissolved in normal saline and administered via intravenous injection at 5 mg/kg, 10 mg/kg, or 20 mg/kg every 8 hours for 3 days. Survival was monitored for 7 days; peritoneal fluid was collected for bacterial load quantification [1]
- Rat pneumonia model: Sprague-Dawley rats were intratracheally inoculated with Pseudomonas aeruginosa (10⁷ CFU/rat). Biapenem (CLI 86815) was dissolved in normal saline and administered via intratracheal injection at 10 mg/kg or 20 mg/kg once daily for 5 days. Rats were sacrificed, and lung tissues were collected for bacterial count and histological analysis [2] |
| ADME/Pharmacokinetics |
In healthy volunteers, the peak plasma concentrations (Cmax) at the end of infusion following intravenous administration of biapenem (CLI 86815) (300 mg and 600 mg) were 14.5 μg/mL (300 mg) and 27.8 μg/mL (600 mg), respectively [4]. The plasma elimination half-life (t1/2) in adults was 1.1–1.3 hours, and in elderly patients (≥65 years) it was 1.5–2.0 hours [4]. Approximately 60–70% of the drug was excreted in the urine within 24 hours, of which approximately 90% was unchanged [1][4]. The drug was well distributed in tissues: the lung tissue/plasma concentration ratio was 1.2, the kidney 5.8, the peritoneal fluid 0.9, and the cerebrospinal fluid (CSF) 0.9. 0.2 (meningitis patients) [4] - Plasma protein binding rate is approximately 3.9-7.0% [1][4]
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| Toxicity/Toxicokinetics |
In vitro experiments showed that biapenem (CLI 86815) at concentrations up to 100 μg/mL was non-cytotoxic to human cells [1]
- In vivo experiments showed that intravenous injection of biapenem (CLI 86815) at doses up to 100 mg/kg in rats for 14 days did not cause significant changes in body weight, organ index, or serum ALT/AST/creatinine levels [1] - Clinical trial data showed that adverse reactions were mild to moderate: gastrointestinal reactions (nausea, diarrhea, 5-8%), rash (2-3%), and elevated liver enzymes (1-2%); no serious nephrotoxicity or neurotoxicity was reported [4] - Acute intravenous LD50 in mice >2000 mg/kg [1] |
| References | |
| Additional Infomation |
Biapenem is a carbapenem antibiotic with a 1-hydroxymethyl ring on its azacyclic butane ring and a pyrrololine ring on its pyrazole-[1,2-a][1,2,4]triazol-6-yl thiosubstituent. It is an antibacterial drug. Biapenem belongs to the carbapenem, pyrazolotriazole, and organosulfur antibiotic classes. Biapenem has been used in clinical trials for the treatment of bacterial infections. Biapenem is a 1-β-methylcarbapenem antibiotic with broad-spectrum antibacterial activity. Its antibacterial activity is similar to imipenem, but it is more stable to human renal dehydropeptidase-1 and has lower neurotoxicity.
Biapenem (CLI 86815) is a synthetic carbapenem antimicrobial drug with broad-spectrum antimicrobial activity[1][2][3][4] - Its antimicrobial mechanism involves binding to bacterial penicillin-binding proteins (especially PBP2 and PBP3), inhibiting bacterial cell wall synthesis, and ultimately leading to bacterial cell lysis[1][3] - It is stable against most β-lactamases and therefore effective against β-lactam-resistant Gram-negative bacteria (except for metallo-β-lactamase-producing strains)[3][4] - Approved indications include community-acquired pneumonia, complicated urinary tract infections, intra-abdominal infections, and skin/soft tissue infections[4] - It is administered intravenously (no oral formulation). It has a good safety profile due to poor oral bioavailability and short-term (7-14 days) use[4] |
| Molecular Formula |
C15H18N4O4S
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| Molecular Weight |
350.39
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| Exact Mass |
350.104
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| Elemental Analysis |
C, 51.42; H, 5.18; N, 15.99; O, 18.26; S, 9.15
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| CAS # |
120410-24-4
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| Related CAS # |
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| PubChem CID |
71339
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| Appearance |
White to off-white solid powder
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| Melting Point |
265-271°C (dec.)
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| Index of Refraction |
1.651
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| LogP |
1.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
609
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S(C1([H])C([H])([H])N2C([H])=NC([H])=[N+]2C1([H])[H])C1=C(C(=O)[O-])N2C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])[C@@]2([H])[C@@]1([H])C([H])([H])[H])=O
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| InChi Key |
MRMBZHPJVKCOMA-WAOAVRLKSA-N
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| InChi Code |
InChI=1S/C15H18N4O4S/c1-7-11-10(8(2)20)14(21)19(11)12(15(22)23)13(7)24-9-3-17-5-16-6-18(17)4-9/h5-11,20H,3-4H2,1-2H3/t7-,8?,10-,11-/m1/s1
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| Chemical Name |
(4R,5S,6S)-3-((6,7-dihydro-5H-pyrazolo[1,2-a][1,2,4]triazol-4-ium-6-yl)thio)-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate
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| Synonyms |
Biapenem; CL 186,815; CL-186,815; CL186,815; L 627; L-627; L627; LJC 10,627; LJC-10,627; LJC10,627; RPX2003; RPX 2003; RPX-2003; Omegacin;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Water : 5~10 mg/mL(~28.54 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 11.11 mg/mL (31.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: PBS: 11.11 mg/mL (31.71 mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8540 mL | 14.2698 mL | 28.5396 mL | |
| 5 mM | 0.5708 mL | 2.8540 mL | 5.7079 mL | |
| 10 mM | 0.2854 mL | 1.4270 mL | 2.8540 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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