| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥ 98%
| ln Vitro |
Lefamulin acetate (0–1 mg/L) exhibits inhibitory activity against M. genitalium, N. gonorrhoeae, and C. trachomatis[2].
Lefamulin acetate has MIC values of ≤0.008 μg/mL, indicating strong activity against all strains of M. pneumoniae[3]. |
|---|---|
| ln Vivo |
Lefamulin (10-140 mg/kg, s.c.) acetate inhibits inflammation in a mouse model of lung neutrophilia caused by lipopolysaccharide [4].
Lefamulin (1.25-160 mg/kg, s.c.) acetate exhibits antimicrobial activity in lung infection-challenged mice challenged with S. pneumoniae or S. aureus[5]. |
| Cell Assay |
Cell Line: C. trachomatis, N. gonorrhoeae, and M. genitalium
Concentration: 0-1 mg/L Incubation Time: Result: demonstrated inhibition of bacterial activity at MIC50s of 0.02 mg/L, 0.063 mg/L, and 0.12 mg/L, in that order. |
| 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 |
C30H49NO7S
|
|---|---|
| Molecular Weight |
567.77756857872
|
| Elemental Analysis |
C, 63.46; H, 8.70; N, 2.47; O, 19.72; S, 5.65
|
| CAS # |
1350636-82-6
|
| Related CAS # |
Lefamulin;1061337-51-6
|
| Appearance |
Solid powder
|
| SMILES |
CC(O)=O.O=C(O[C@@H]1C[C@](C=C)(C)[C@@H](O)[C@H](C)[C@]2(CCC3=O)[C@]3([H])[C@@]1(C)[C@H](C)CC2)CS[C@H]4[C@H](O)C[C@H](N)CC4
|
| InChi Key |
WSMXIQXWHPSVDE-ZPJPNJFZSA-N
|
| InChi Code |
InChI=1S/C28H45NO5S.C2H4O2/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)281-2(3)4/h6,16-18,20-22,24-25,31,33H,1,7-15,29H2,2-5H31H3,(H,3,4)/t16-,17+,18-,20-,21-,22-,24+,25+,26-,27+,28+/m1./s1
|
| 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 acetic acid (1:1)
|
| Synonyms |
BC3781.Ac; BC-3781; BC 3781; BC3781; Xenleta;BC-3781.Ac; BC 3781.Ac;
|
| 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: 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (176.12 mM )
Ethanol : ~100 mg/mL H2O : 1~100 mg/mL (~1.76 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.40 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 25.0 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: 2.5 mg/mL (4.40 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (4.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+90% (20% SBE-β-CD in Saline): 2.5 mg/mL (4.40 mM) Solubility in Formulation 5: 100 mg/mL (176.12 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7612 mL | 8.8062 mL | 17.6125 mL | |
| 5 mM | 0.3522 mL | 1.7612 mL | 3.5225 mL | |
| 10 mM | 0.1761 mL | 0.8806 mL | 1.7612 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
COA