| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
- Mezlocillin sodium exerts antibacterial effects by targeting bacterial penicillin-binding proteins (PBPs), which are key enzymes involved in bacterial cell wall synthesis[2]
|
|---|---|
| ln Vitro |
- Antibacterial activity against gram-positive bacteria: Mezlocillin sodium showed inhibitory effects on various gram-positive bacteria. The minimum inhibitory concentration (MIC) against penicillin-susceptible Staphylococcus aureus was 0.25–1 μg/ml, and against Streptococcus pneumoniae was 0.125–0.5 μg/ml[2]
- Antibacterial activity against gram-negative bacteria: Mezlocillin sodium exhibited broad-spectrum activity against gram-negative bacteria. Its MIC against Escherichia coli was 1–4 μg/ml, against Klebsiella pneumoniae was 2–8 μg/ml, and against Pseudomonas aeruginosa was 4–16 μg/ml[2] - Immunomodulatory effect on lymphocytes: In vitro, Mezlocillin sodium at a concentration of 100 μg/ml inhibited phytohemagglutinin (PHA)-induced proliferation of human peripheral blood lymphocytes (measured by 3H-thymidine incorporation assay). It had no significant effect on lymphocyte proliferation without PHA stimulation[1] - Effect on monocyte cytokine release: Mezlocillin sodium (100 μg/ml) did not significantly alter lipopolysaccharide (LPS)-induced release of tumor necrosis factor-α (TNF-α) or interleukin-1 (IL-1) from human monocytes in vitro[1] |
| ln Vivo |
Medlocillin subcutaneous injection (1.7-5.7 mg/kg; twice daily; 7 days) was used as an in vivo treatment to decrease IgM and IgG responses, delayed-type hypersensitivity reactions, hair loss, and lymphocyte proliferation dose[1].
- Accidental high-dose intraventricular administration in humans: A patient accidentally received an intraventricular injection of 2 g Mezlocillin sodium (concentration: 200 mg/ml) instead of the intended intrathecal medication. Within 10 minutes, the patient developed generalized tonic-clonic seizures and decreased consciousness (Glasgow Coma Scale score: 6). Cerebrospinal fluid (CSF) exchange was performed as treatment: ~10–15 ml of CSF was removed and replaced with sterile normal saline every 15–30 minutes, totaling ~100 ml of CSF exchanged. The patient’s seizures ceased 6 hours after treatment, and consciousness gradually recovered to normal within 48 hours.[3] |
| Cell Assay |
- Lymphocyte proliferation assay: Human peripheral blood lymphocytes were isolated from healthy donors and suspended in culture medium. The cells were divided into three groups: control group (no stimulation), PHA-stimulated group (5 μg/ml PHA), and PHA + Mezlocillin sodium group (5 μg/ml PHA + 100 μg/ml Mezlocillin sodium). All groups were incubated at 37°C in a 5% CO₂ atmosphere for 72 hours. During the last 18 hours of incubation, 3H-thymidine was added to each well. The amount of 3H-thymidine incorporated into DNA was measured using a liquid scintillation counter to assess lymphocyte proliferation[1]
- In vitro antibacterial susceptibility assay (broth dilution method): Bacterial strains (including gram-positive and gram-negative species) were cultured to the logarithmic growth phase and adjusted to a concentration of 1×10⁶ colony-forming units (CFU)/ml. Serial two-fold dilutions of Mezlocillin sodium (ranging from 0.0625 to 128 μg/ml) were prepared in Mueller-Hinton broth. Equal volumes of bacterial suspension and drug dilutions were mixed, then incubated at 37°C for 18–24 hours. The MIC was defined as the lowest concentration of Mezlocillin sodium that completely inhibited bacterial growth (no visible turbidity)[2] |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse [1]
Doses: 1.7, 4.3, and 5.7 mg/kg Route of Administration: subcutaneous injection; 1.7, 4.3, and 5.7 mg/kg; twice (two times) daily; 7-day Experimental Results: All dose treatments were Inhibits IgM and IgG responses as well as delayed-type hypersensitivity reactions. Hair loss was observed in most animals treated at all doses. Inhibits lymphocyte proliferation in animal spleen cell cultures. |
| Toxicity/Toxicokinetics |
Acute toxicity caused by accidental high-dose intraventricular administration: One patient developed acute neurotoxicity, including generalized tonic-clonic seizures and severe altered consciousness (Glasgow Coma Scale score: 6), after intraventricular injection of 2 g mezlocillin sodium (200 mg/mL). The toxicity was reversible after cerebrospinal fluid replacement therapy, and no long-term adverse reactions were observed. [3]
|
| References |
[1]. Roszkowski W, et al. Antibiotics and immunomodulation: effects of cefotaxime, amikacin, mezlocillin, piperacillin and clindamycin. Med Microbiol Immunol. 1985;173(5):279-89.
[2]. Bodey GP, et al. Mezlocillin: in vitro studies of a new broad-spectrum penicillin. Antimicrob Agents Chemother. 1977 Jan;11(1):74-9. [3]. Kristof RA, et al. Treatment of accidental high dose intraventricular mezlocillin application by cerebrospinal fluid exchange. J Neurol Neurosurg Psychiatry. 1998 Mar;64(3):379-81. |
| Additional Infomation |
Mezlocillin sodium is an organic sodium salt. It contains a Mezlocillin (1-) group. It is a semi-synthetic ampicillin derivative belonging to the acylurea penicillin class. It has been proposed for the treatment of certain anaerobic bacterial infections and may be effective against inner ear, bile, and central nervous system infections. Mezlocillin sodium is a broad-spectrum penicillin antibiotic characterized by its effectiveness against both Gram-positive and Gram-negative bacteria [2]. Mezlocillin sodium has selective immunomodulatory effects: it inhibits only mitogen (PHA)-induced lymphocyte proliferation without affecting basal lymphocyte activity or monocyte cytokine release [1].
|
| Molecular Formula |
C21H24NAN5O8S2
|
|---|---|
| Molecular Weight |
561.56
|
| Exact Mass |
561.096
|
| CAS # |
42057-22-7
|
| Related CAS # |
Mezlocillin;51481-65-3
|
| PubChem CID |
23685177
|
| Appearance |
White to off-white solid powder
|
| LogP |
0.107
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
37
|
| Complexity |
1090
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC([C@H](NC(N3CCN(S(=O)(C)=O)C3=O)=O)C4=CC=CC=C4)=O)N1C2=O)[O-].[Na+]
|
| InChi Key |
GTGQRSIMEUWHPA-ZBJAFUORSA-M
|
| InChi Code |
InChI=1S/C21H25N5O8S2.Na/c1-21(2)14(18(29)30)26-16(28)13(17(26)35-21)22-15(27)12(11-7-5-4-6-8-11)23-19(31)24-9-10-25(20(24)32)36(3,33)34;/h4-8,12-14,17H,9-10H2,1-3H3,(H,22,27)(H,23,31)(H,29,30);/q;+1/p-1/t12-,13-,14+,17-;/m1./s1
|
| Chemical Name |
sodium;(2S,5R,6R)-3,3-dimethyl-6-[[(2R)-2-[(3-methylsulfonyl-2-oxoimidazolidine-1-carbonyl)amino]-2-phenylacetyl]amino]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~445.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7808 mL | 8.9038 mL | 17.8075 mL | |
| 5 mM | 0.3562 mL | 1.7808 mL | 3.5615 mL | |
| 10 mM | 0.1781 mL | 0.8904 mL | 1.7808 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
