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| 1mg |
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| Targets |
JB-95 acetate targets the outer membrane of E. coli, specifically interacting with selected beta-barrel outer membrane proteins, including the essential proteins BamA and LptD [3L10-L12]. By binding to these targets, JB-95 acetate disrupts the integrity of the outer membrane. Unlike traditional antibiotics, it does not target an intracellular enzyme or receptor but a structural component of the bacterial cell envelope.
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| ln Vitro |
In cell-free assays, JB-95 acetate is evaluated for its ability to disrupt isolated E. coli outer membranes. The interaction with target proteins can be studied using surface plasmon resonance (SPR) to determine binding affinity to purified BamA or LptD. However, as an antibacterial peptide, its primary activity is assessed in whole-cell systems rather than traditional enzyme inhibition assays.
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| ln Vivo |
JB-95 acetate exhibits potent antimicrobial activity against E. coli with minimum inhibitory concentrations (MICs) in the low micromolar to nanomolar range [16L5-L7]. In cell culture, the peptide selectively damages the bacterial outer membrane as visualized by electron microscopy and fluorescence studies, without affecting the inner membrane or causing cellular lysis [14L8-L10]. The compound is active against both laboratory and clinical E. coli strains.
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| Enzyme Assay |
The outer membrane disruption assay is performed using isolated E. coli outer membrane vesicles or whole cells. The effect of JB-95 acetate on membrane integrity is measured by assessing the uptake of membrane-impermeable fluorescent probes like 1-N-phenylnaphthylamine (NPN). An increase in fluorescence indicates outer membrane permeabilization. The assay is conducted in 96-well plates with a fluorescence reader, and data is expressed as a percentage of control.
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| Cell Assay |
E. coli cultures are grown to mid-log phase in LB or MH broth. JB-95 acetate is added at concentrations ranging from 0.1 to 100 uM, and cultures are incubated for 2-4 hours at 37degC. Outer membrane disruption is assessed by NPN uptake fluorescence, while cell viability is measured by colony-forming unit (CFU) counting. Bacterial morphology is examined by scanning and transmission electron microscopy after 1 hour of treatment. Controls include untreated cells and a known membrane-disrupting agent.
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| Animal Protocol |
In a mouse model of E. coli septicemia or peritonitis, JB-95 acetate has been evaluated for in vivo efficacy [17L4-L6]. The compound is administered via intraperitoneal injection (e.g., 5-20 mg/kg) at the time of bacterial challenge. The primary endpoint is animal survival over 7-14 days. Bacterial load in blood, peritoneal fluid, and organs (liver, spleen) is quantified by CFU counts. Treatment with JB-95 acetate significantly reduces bacterial burden compared to vehicle control.
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| ADME/Pharmacokinetics |
JB-95 acetate is a macrocyclic peptide with a molecular weight of 1971.41 Da (free base) [8L15-L16]. It is soluble in water at ≥50 mg/mL. As a peptide, it has a short plasma half-life (minutes) due to rapid proteolytic degradation and renal clearance. For in vivo studies, it is formulated in a solution containing DMSO, PEG300, Tween 80, and saline, or directly in sterile water. The compound is stored as a powder at -20degC under nitrogen and away from moisture and light [8L18-L19].
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| Toxicity/Toxicokinetics |
JB-95 acetate is generally well-tolerated at antibacterial doses in animal models. Its selectivity for the outer membrane of E. coli without disrupting the inner membrane of mammalian cells suggests a favorable toxicity profile. In cell culture, no significant cytotoxicity is observed at concentrations that are effective against bacteria. Standard laboratory safety precautions (gloves, lab coat) should be followed as the compound may be a skin/eye irritant. No formal clinical toxicology data is available.
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| References |
[1]. Urfer M, et, al. A Peptidomimetic Antibiotic Targets Outer Membrane Proteins and Disrupts Selectively the Outer Membrane in Escherichia coli. J Biol Chem. 2016 Jan 22;291(4):1921-1932.
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| Additional Infomation |
JB-95 acetate is a research-use-only peptidomimetic antibiotic discovered through a novel approach targeting the outer membrane of Gram-negative bacteria [14L4-L10]. It has not been approved for clinical use. Its unique mechanism, involving disruption of the outer membrane via binding to BamA and LptD, opens new avenues for antibiotic development against resistant E. coli strains [3L10-L12]. The compound is supplied as a powder (C92H151N35O14.xC2H4O2) and should be stored sealed under nitrogen, protected from light. It is for laboratory use only and not for human therapeutic applications.
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| Molecular Formula |
C92H151N35O14.XC2H4O2
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| Molecular Weight |
1971.41 (free base)
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| Appearance |
White to off-white solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
H2O :≥ 50 mg/mL
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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.) |
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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