| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Peptidoglycan cross-linking pentaglycine bridges in Staphylococcus aureus cell walls [1]
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|---|---|
| ln Vitro |
Lysostaphin exhibited potent bactericidal activity against S. aureus strains including MRSA (MSSA MIC: 0.001–0.003 μg/mL; MRSA MIC: 0.002–0.008 μg/mL). Time-kill assays showed ≥3-log10 CFU reduction within 15 min at 1× MIC. No activity against coagulase-negative staphylococci or other Gram-positive bacteria was observed. [1]
Atomic force microscopy revealed cell wall digestion within 15 min: initial pore formation (50-200 nm diameter) progressing to complete lysis by 60 min at 10 μg/mL. Zymogram analysis confirmed specific cleavage of pentaglycine bridges. [3] |
| ln Vivo |
Lysostaphin exhibited potent bactericidal activity against S. aureus strains including MRSA (MSSA MIC: 0.001–0.003 μg/mL; MRSA MIC: 0.002–0.008 μg/mL). Time-kill assays showed ≥3-log10 CFU reduction within 15 min at 1× MIC. No activity against coagulase-negative staphylococci or other Gram-positive bacteria was observed. [1]
Atomic force microscopy revealed cell wall digestion within 15 min: initial pore formation (50-200 nm diameter) progressing to complete lysis by 60 min at 10 μg/mL. Zymogram analysis confirmed specific cleavage of pentaglycine bridges. [3] |
| Enzyme Assay |
Zymogram analysis: S. aureus cell walls were incorporated into SDS-PAGE gels. After electrophoresis, gels were renatured in Triton X-100 solution and incubated in 50 mM Tris-HCl (pH 7.5) at 37°C for 16 h. Clear zones indicated peptidoglycan hydrolase activity. [3]
MIC determination: Broth microdilution per CLSI guidelines with cation-adjusted Mueller-Hinton broth. Lysostaphin serially diluted (0.0005–128 μg/mL), inoculated with 5×105 CFU/mL bacteria, incubated 18-24 h at 35°C. [1] |
| Animal Protocol |
Zymogram analysis: S. aureus cell walls were incorporated into SDS-PAGE gels. After electrophoresis, gels were renatured in Triton X-100 solution and incubated in 50 mM Tris-HCl (pH 7.5) at 37°C for 16 h. Clear zones indicated peptidoglycan hydrolase activity. [3]
MIC determination: Broth microdilution per CLSI guidelines with cation-adjusted Mueller-Hinton broth. Lysostaphin serially diluted (0.0005–128 μg/mL), inoculated with 5×105 CFU/mL bacteria, incubated 18-24 h at 35°C. [1] |
| ADME/Pharmacokinetics |
In mice, IV administered lysostaphin (5 mg/kg) showed:
- Distribution half-life (t1/2α): 0.13 h
- Elimination half-life (t1/2β): 1.2 h
- Plasma clearance: 0.45 L/h/kg
- Volume of distribution: 0.75 L/kg
No detectable metabolism; renal excretion predominant. [2]
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| Toxicity/Toxicokinetics |
No acute toxicity at 160 mg/kg IV (highest tested dose) in mice. No histopathological changes in kidneys/liver. Transient elevation of anti-lysostaphin antibodies after repeated dosing without neutralizing activity. [2]
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| References | |
| Additional Infomation |
Lysostaphin is a zinc-dependent glycyl-glycine endopeptidase produced by Staphylococcus simulans, specifically cleaving pentaglycine cross-bridges in S. aureus peptidoglycan. [1]
Clinical potential for MRSA infections: Rapid bactericidal action and synergy with β-lactams observed. Resistance development rare (<10-9 frequency at 4× MIC). [3] A 25-kDa peptidase produced by Staphylococcus simulans which cleaves a glycine-glcyine bond unique to an inter-peptide cross-bridge of the STAPHYLOCOCCUS AUREUS cell wall. |
| Molecular Formula |
C74H112CL2N6O11
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|---|---|
| Molecular Weight |
1332.62069988251
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| Exact Mass |
282.1
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| CAS # |
9011-93-2
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| PubChem CID |
167312533
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
483.6±55.0 °C at 760 mmHg
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| Flash Point |
246.3±31.5 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.618
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| LogP |
2.18
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
15
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
93
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| Complexity |
2150
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(=C(C=C(C=1)COC(N1C=CC2=C1N=CN=C2N(C)C1CN(C(CC#N)=O)CCC1C)=O)Cl)OC(CC(C)CCCC(C)CC(=O)OC(COC(CCCCCCCC=CCCCCCCCC)=O)COC(CCCCCCCC=CCCCCCCCC)=O)=O
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| InChi Key |
JITWMWVPQUZNBO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C74H112Cl2N6O11/c1-7-9-11-13-15-17-19-21-23-25-27-29-31-33-35-40-67(84)89-54-61(55-90-68(85)41-36-34-32-30-28-26-24-22-20-18-16-14-12-10-8-2)92-69(86)48-57(3)38-37-39-58(4)49-70(87)93-71-63(75)50-60(51-64(71)76)53-91-74(88)82-47-44-62-72(78-56-79-73(62)82)80(6)65-52-81(46-43-59(65)5)66(83)42-45-77/h21-24,44,47,50-51,56-59,61,65H,7-20,25-43,46,48-49,52-55H2,1-6H3
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| Chemical Name |
1-O-[2,6-dichloro-4-[[4-[[1-(2-cyanoacetyl)-4-methylpiperidin-3-yl]-methylamino]pyrrolo[2,3-d]pyrimidine-7-carbonyl]oxymethyl]phenyl] 9-O-[1,3-di(octadec-9-enoyloxy)propan-2-yl] 3,7-dimethylnonanedioate
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| Synonyms |
Lysostaphin - from Staphylococcus staphylolyticus; 58856-93-2; Zymosan A; Lysostaphin - from Staphylococcus staphylolyticus; 1-O-[1,3-bis[[(Z)-octadec-9-enoyl]oxy]propan-2-yl] 9-O-[2,6-dichloro-4-[[4-[[(3R,4R)-1-(2-cyanoacetyl)-4-methylpiperidin-3-yl]-methylamino]pyrrolo[2,3-d]pyrimidine-7-carbonyl]oxymethyl]phenyl] 3,7-dimethylnonanedioate;
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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, avoid exposure to moisture. |
| 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 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7504 mL | 3.7520 mL | 7.5040 mL | |
| 5 mM | 0.1501 mL | 0.7504 mL | 1.5008 mL | |
| 10 mM | 0.0750 mL | 0.3752 mL | 0.7504 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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