Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
MIC50: 0.12 mg/L(P. aeruginosa)[2] MIC90: 0.12 mg/L(P. aeruginosa)[2] IC50: 5.84 μM (gentamicin)[2]
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ln Vitro |
Murepavadin is active against P. aeruginosa, as evidenced by its 0.12 mg/L MIC50 and MIC90 values[2]. With an IC50 value of 5.84 μM, murepavadin inhibits the absorption of gentamicin by megalin in vitro[2].
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ln Vivo |
In preclinical animal models, including infection with XDR isolates, murepavadin (sc; 0-100 mg/kg) is effective [2].
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Animal Protocol |
Animal/Disease Models: Murine models of P. aeruginosa infection[2]
Doses: 0-100 mg/kg Route of Administration: Subcutaneous, q24h or q12h Experimental Results: Resulted in an increase in survival rate to 100% and demonstrated Dramatically lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection. Animal/Disease Models: Mouse, rat, rabbit, and monkey[2] Doses: 0-5 mg/kg Route of Administration: intraperitoneal (ip)or subcutaneous, single Experimental Results: Followed a two-compartment model following intravenous (iv) administration and decline of plasma concentrations. Distributed into the aqueous phase of the body, and systemic plasma clearance (CL) values were similar to the species-specific glomerular filtration rates (GFRs) . Had high bioavailability (67.79 %) after subcutaneous (sc) administration in rats but had low oral bioavailability (<0.01%). Had a linear relationship between ELF AUC and unbound plasma AUC in mouse. Did not readily cross the blood/brain barrier. |
References |
[1]. Matteo Bassetti, et al. New antibiotics for ventilator-associated pneumonia. Curr Opin Infect Dis. 2018 Jan 13.
[2]. Ignacio Martin-Loeches, et al. Murepavadin: a new antibiotic class in the pipeline. Expert Rev Anti Infect Ther. 2018 Apr;16(4):259-268. |
Molecular Formula |
C73H112N22O16.C2HF3O2
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Molecular Weight |
1667.83
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Related CAS # |
Murepavadin;944252-63-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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 Vitro) |
H2O :~50 mg/mL (~29.98 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 25 mg/mL (14.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with heating and sonication.
 (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 0.5996 mL | 2.9979 mL | 5.9958 mL | |
5 mM | 0.1199 mL | 0.5996 mL | 1.1992 mL | |
10 mM | 0.0600 mL | 0.2998 mL | 0.5996 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.