Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Lefamulin (formerly also known as BC-3781; Xenleta) is a semi-synthetic, oral pleuromutilin antibiotic approved to treat adults with community-acquired bacterial pneumonia. It potently inhibits the synthesis of bacterial protein, which is required for bacteria to grow. Lefamulin acts by binding to the peptidyl transferase center, or PTC, on the bacterial ribosome in such a way that it interferes with the interaction of protein production at two key sites known as the 'A' site and the 'P' site, resulting in the inhibition of bacterial proteins and the cessation of bacterial growth. Lefamulin's binding occurs with high affinity, high specificity and at molecular sites that are different than other antibiotic classes. Lefamulin exhibited MIC50 and MIC90 values of 0.12 and 0.25 μg/ml, respectively, against the entire collection (n = 822). Similar results were obtained for lefamulin against each of the most common serotypes as well as against multidrug-resistant isolates and strains that are nonsusceptible to ceftriaxone or erythromycin. Lefamulin may be useful for the treatment of community-acquired respiratory tract infections.
ln Vitro |
Lefamulin (0–1 mg/L) inhibits the growth of N. gonorrhoeae, M. genitalium, and C. trachomatis[2].
With MIC values of less than 0.008 μg/mL, lefamulin exhibits strong activity against every strain of M. pneumoniae[3]. |
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ln Vivo |
Lefamulin (10–140 mg/kg, s.c.) reduces inflammation in a mouse model of lung neutrophilia caused by lipopolysaccharide (LPS)[4].
In mice with lung infections caused by S. pneumoniae or S. aureus, lefamulin (1.25-160 mg/kg, s.c.) exhibits antibacterial activity[5]. |
Cell Assay |
Cell Line: C. trachomatis, N. gonorrhoeae, and M. genitalium
Concentration: 0-1 mg/L Incubation Time: Result: MIC50s of 0.02 mg/L, 0.063 mg/L, and 0.12 mg/L, respectively, were used to inhibit bacterial activity. |
Animal Protocol |
Animal Model: LPS-induced lung neutrophilia mouse model[4]
Dosage: 10-140 mg/kg Administration: Subcutaneous injection (s.c.) Result: decreased numbers of BALF neutrophil cells. Diminished levels of MMP-9, chemokines (CXCL-1, CXCL-2, and CCL-2) and pro-inflammatory cytokines (TNF-α, IL-6, IL-1β, and GM-CSF) in mouse lung tissue. |
References |
Molecular Formula |
C28H45NO5S
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Molecular Weight |
507.725607633591
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Exact Mass |
507.30
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Elemental Analysis |
C, 66.24; H, 8.93; N, 2.76; O, 15.76; S, 6.31
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CAS # |
1061337-51-6
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Related CAS # |
Lefamulin acetate;1350636-82-6
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Appearance |
Solid powder
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SMILES |
O=C(O[C@H]1[C@@]([C@H](C)CC2)(C)[C@@](C(CC3)=O)([H])[C@]32[C@@H](C)[C@H](O)[C@](C)(C=C)C1)CS[C@H]4[C@H](O)C[C@H](N)CC4
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InChi Key |
KPVIXBKIJXZQJX-FCEONZPQSA-N
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InChi Code |
InChI=1S/C28H45NO5S/c1-6-26(4)14-22(34-23(32)15-35-21-8-7-18(29)13-20(21)31)27(5)16(2)9-11-28(17(3)25(26)33)12-10-19(30)24(27)28/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H3/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27+,28+/m1/s1
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Chemical Name |
(3aR,4R,5R,7S,8S,9R,9aS,12R)-8-hydroxy-4,7,9,12-tetramethyl-3-oxo-7-vinyldecahydro-4,9a-propanocyclopenta[8]annulen-5-yl 2-(((1R,2R,4R)-4-amino-2-hydroxycyclohexyl)thio)acetate
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Synonyms |
BC-3781; BC 3781; BC3781
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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 | 1.9696 mL | 9.8478 mL | 19.6955 mL | |
5 mM | 0.3939 mL | 1.9696 mL | 3.9391 mL | |
10 mM | 0.1970 mL | 0.9848 mL | 1.9696 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.