| Size | Price | |
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| 25mg | ||
| 50mg | ||
| 100mg | ||
| 250mg | ||
| Other Sizes |
| Targets |
Bacterial ribosome and Release Factor (RF). Api137 binds simultaneously to the ribosomal polypeptide exit tunnel (near the peptidyl transferase center) and to the release factor (RF), specifically RF-2. This dual binding depletes the cellular RF pool and leads to ribosomal arrest at stop codons, effectively inhibiting protein translation.
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| ln Vitro |
Api137 inhibits bacterial growth with MICs in the low micromolar range against a broad spectrum of Gram-negative pathogens, including ESKAPE pathogens. It disrupts the proper assembly of the large (50S) ribosomal subunit. The peptide induces ribosome stalling at stop codons, which is a distinct mechanism from many other ribosome-targeting antibiotics.
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| ln Vivo |
In murine models of systemic infection, Api137 significantly improves survival. It has been tested in models of peritonitis/sepsis caused by E. coli. Intraperitoneal administration of Api137 leads to rapid bacterial clearance, reduced inflammatory cytokine levels, and improved survival rates compared to vehicle-treated controls. It shows low toxicity in vivo at therapeutically effective doses.
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| Enzyme Assay |
A cell-free transcription-translation (TX-TL) assay using bacterial lysates (e.g., E. coli S30 extract) and a luciferase reporter plasmid is performed. Api137 is added at varying concentrations (0.1-50 uM), and luciferase activity is measured after 60-90 minutes. This system directly quantifies the effect of the peptide on translation machinery independent of cell uptake, confirming its direct ribosome-binding mechanism.
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| Cell Assay |
Minimum Inhibitory Concentration (MIC) is determined by broth microdilution in 96-well plates according to CLSI guidelines. Bacterial strains (E. coli, K. pneumoniae, P. aeruginosa) are grown in Mueller-Hinton broth (MHB) and incubated with serial dilutions of Api137 (0.125-64 ug/mL) at 37degC for 18-24 hours. The MIC is the lowest concentration with no visible bacterial growth. Colony-forming units (CFU) are also quantified.
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| Animal Protocol |
Female BALB/c mice (6-8 weeks) are injected intraperitoneally (IP) with a lethal dose of E. coli (e.g., ATCC 25922, ~1-2 × 10^8 CFU). One hour post-infection, Api137 is administered intravenously or IP (doses range: 1-20 mg/kg). Survival is monitored for 5-7 days. Bacterial loads in blood, peritoneum, and spleen are quantified by CFU plating at 6-24 hours post-infection. Cytokine levels are measured by ELISA.
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| ADME/Pharmacokinetics |
Peptide antibiotics typically have a short plasma half-life (30-60 minutes) due to renal filtration and proteolytic degradation. Api137 exhibits moderate plasma stability, with some activity retained after 2-4 hours in murine serum. It is administered intravenously or IP for in vivo studies due to low oral bioavailability. Its primary route of elimination is renal.
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| Toxicity/Toxicokinetics |
Api137 demonstrates low hemolytic activity against human red blood cells (EC50 > 200 uM) and low cytotoxicity against mammalian cell lines (e.g., HEK293, HepG2) at therapeutic concentrations (IC50 > 50 uM). In animal studies, no significant weight loss, hepatotoxicity (ALT/AST), or nephrotoxicity (creatinine/BUN) was observed at effective doses.
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| References |
[1]. Florin T, et, al. An antimicrobial peptide that inhibits translation by trapping release factors on the ribosome. Nat Struct Mol Biol. 2017 Sep;24(9):752-757.
[2]. Graf M, et, al. Intracellular Antimicrobial Peptides Targeting the Protein Synthesis Machinery. Adv Exp Med Biol. 2019:1117:73-89. [3]. Knappe D, et, al. Continuous Subcutaneous Delivery of Proline-Rich Antimicrobial Peptide Api137 Provides Superior Efficacy to Intravenous Administration in a Mouse Infection Model. Front Microbiol. 2019 Oct 2:10:2283. |
| Additional Infomation |
Api137 was discovered by researchers at the University of Bonn, Germany. Its unique dual mechanism of action (targeting both the ribosome and release factor) makes it a highly innovative antibiotic candidate. Because it targets the translation machinery in a novel way, Api137 circumvents many common mechanisms of antibiotic resistance. This peptide is still in preclinical development and has not yet entered human clinical trials. No FDA approval.
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| Molecular Formula |
C104H171N37O22
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|---|---|
| Molecular Weight |
2291.71
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| Sequence |
TMG-Orn-Asn-Asn-Arg-Pro-Val-Tyr-Ile-Pro-Arg-Pro-Arg-Pro-Pro-His-Pro-Arg-Leu
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| Appearance |
Typically exists as solid at room temperature
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4364 mL | 2.1818 mL | 4.3636 mL | |
| 5 mM | 0.0873 mL | 0.4364 mL | 0.8727 mL | |
| 10 mM | 0.0436 mL | 0.2182 mL | 0.4364 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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