| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
At concentrations below 1 μg/ml, 90% of strains of Salmonella spp., Haemophilus influenzae, Klebsiella spp., Proteus spp., Morganella spp., Neisseria gonorrhoeae, Neisseria meningitidis, and Escherichia coli are inhibited by clavulanam (Latamoxef) [1]. Acinetobacter is typically resistant to moxalactam, while moxalactam shows modest effectiveness against Pseudomonas aeruginosa and is generally active against other Pseudomonas species [1]. Mosalactam inhibits the synthesis of β-lactamases, does not induce class I β-lactamases, and demonstrates significant in vitro stability against a variety of β-lactamases, including those produced by Bacteroides fragilis. lactamase [1].
|
|---|---|
| ln Vivo |
Mice with bacterial infections respond well to latamoxef (0–7.4 mg/mouse; subcutaneous injection; once) [2].
|
| Animal Protocol |
Animal/Disease Models: 4weeks old male strain ICR mouse, weight 18-20 g, bacterial infection model [2]
Doses: 0-7.4 mg/mouse Route of Administration: subcutaneous injection, one time Experimental Results:shows protective activity, ED50 is less than 7.4 mg /mouse Targets mice infected with Gram-positive and Gram-negative bacteria. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Rapidly absorbed after oral administration. 75% excreted by the kidneys. 8.51 L/h Biological half-life 1.6 hours |
| Toxicity/Toxicokinetics |
Protein Binding
40% |
| References |
|
| Additional Infomation |
Moxalactam is a broad-spectrum oxacon antibiotic, its oxazine ring substituted with tetrazolium thiomethyl, and its azazobutanone ring with methoxy and 2-carboxy-2-(4-hydroxyphenyl)acetamido substituents. It is an antibacterial drug. It belongs to the oxacon and cephalosporin classes. Latamoxifen is a broad-spectrum β-lactam antibiotic, its structure similar to cephalosporins, the difference being that in some cephalosporin compounds, the thiazole bicyclic moiety is substituted with the oxazona bicyclic moiety. Because latamoxiv can cross the blood-brain barrier, it is particularly recommended for the treatment of meningitis and anaerobic bacterial infections. Latamoxifen has been reported in the Chinese honeybee (Apis cerana), and relevant data are available. Moxalactam is a semi-synthetic oxacon β-lactam antibiotic with antibacterial activity, primarily used against Gram-negative aerobic bacteria. Replacing the sulfur atom on the β-lactam ring with an oxygen atom and introducing a methyltetrazole thio group and a p-hydroxyphenylmalonyl group enhances the antibacterial activity of mosalatin. The 7α-methoxy and p-hydroxyphenylmalonyl groups improve the drug's stability against β-lactamases. Use of this drug has been associated with fatal bleeding events. Latamoxifen is a broad-spectrum β-lactam antibiotic with a structure similar to cephalosporins, the difference being that the thiazole bicyclic moiety in some cephalosporins is replaced by an oxazabicyclic moiety. Due to its ability to cross the blood-brain barrier, it is particularly recommended for the treatment of meningitis and anaerobic infections.
Drug Indications Latamoxifen is an oxazacephalosporin antibiotic, usually classified with cephalosporins. It is used to treat bacterial infections. Latamoxifen is mainly used to treat bone and joint infections, gastrointestinal infections, gynecological infections, meningitis, respiratory infections, sepsis, skin infections, soft tissue infections, and urinary tract infections. Mechanism of Action Penicillin drugs work by opening the lactam ring, acylating the C-terminal domain of penicillin-sensitive transpeptidase (penicillin-binding protein). Inactivation of this enzyme prevents the formation of cross-links between two linear peptidoglycan chains, thereby inhibiting the third (and final) stage of bacterial cell wall synthesis. Subsequently, bacterial cell wall autolysins (such as autolysins) mediate cell lysis; amoxicillin may interfere with the action of autolysin inhibitors. Pharmacodynamics Latamoxifen works by inhibiting bacterial cell wall biosynthesis. |
| Molecular Formula |
C20H20N6O9S
|
|---|---|
| Molecular Weight |
520.47
|
| Exact Mass |
520.101
|
| CAS # |
64952-97-2
|
| Related CAS # |
Moxalactam sodium salt;64953-12-4
|
| PubChem CID |
47499
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.77 g/cm3
|
| Boiling Point |
836ºC
|
| Melting Point |
117 - 122ºC
|
| Index of Refraction |
1.768
|
| LogP |
-0.6
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
13
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
36
|
| Complexity |
958
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CN1C(SCC2=C(N3C([C@](NC([C@H](C(O)=O)C4=CC=C(O)C=C4)=O)(OC)[C@H]3OC2)=O)C(O)=O)=NN=N1
|
| InChi Key |
JWCSIUVGFCSJCK-CAVRMKNVSA-N
|
| InChi Code |
InChI=1S/C20H20N6O9S/c1-25-19(22-23-24-25)36-8-10-7-35-18-20(34-2,17(33)26(18)13(10)16(31)32)21-14(28)12(15(29)30)9-3-5-11(27)6-4-9/h3-6,12,18,27H,7-8H2,1-2H3,(H,21,28)(H,29,30)(H,31,32)/t12?,18-,20+/m1/s1
|
| Chemical Name |
(6R,7R)-7-[[2-carboxy-2-(4-hydroxyphenyl)acetyl]amino]-7-methoxy-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-oxa-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 1.9213 mL | 9.6067 mL | 19.2134 mL | |
| 5 mM | 0.3843 mL | 1.9213 mL | 3.8427 mL | |
| 10 mM | 0.1921 mL | 0.9607 mL | 1.9213 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.