| Identification | Back Directory | [Name]
Lemborexant | [CAS]
944252-63-5 | [Synonyms]
POL7080
POL-7080
POL 7080
PubChem ID: 91824766
Murepavadin (POL7080)
POL7080;MUREPAVADIN;POL-7080;POL 7080
Cyclo[L-alanyl-L-seryl-D-prolyl-L-prolyl-L-threonyl-L-tryptophyl-L-isoleucyl-(2S)-2,4-diaminobutanoyl-L-ornithyl-(2R)-2,4-diaminobutanoyl-(2S)-2,4-diaminobutanoyl-L-tryptophyl-(2S)-2,4-diaminobutanoyl-(2S)-2,4-diaminobutanoyl] | [Molecular Formula]
C73H112N22O16 | [MDL Number]
MFCD32214888 | [MOL File]
944252-63-5.mol | [Molecular Weight]
1553.84 |
| Chemical Properties | Back Directory | [Boiling point ]
1894.3±65.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [pka]
12.90±0.70(Predicted) | [Sequence]
cyclo[Ala-Ser-D-Pro-Pro-Thr-Trp-Ile-Dab-Orn-D-Dab-Dab-Trp-Dab-Dab] | [InChIKey]
RIDRXGOBXZLKHZ-DLVLNFPJNA-N |
| Hazard Information | Back Directory | [Uses]
Murepavadin (POL7080), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic. Murepavadin exhibits a potent antimicrobial activity for P. aeruginosa with both MIC50 and MIC90 values of 0.12 mg/L. Murepavadin also can target the lipopolysaccharide transport portin D. Murepavadin can be used for the research of bacterial resistance[1][2]. | [in vivo]
Murepavadin (s.c.; 0-100 mg/kg) is active in pre-clinical animal models including infections with XDR isolates[2]. | Animal Model: | murine models of P. aeruginosa infection[2] | | Dosage: | 0-100 mg/kg | | Administration: | Subcutaneous, q24h or q12h | | Result: | Resulted in an increase in survival rate to 100% and showed significantly lower CFU levels both in the blood and in the peritoneal fluid at 2 and 10 mg/kg 1 h post-infection. |
| Animal Model: | Mouse, rat, rabbit, and monkey[2] | | Dosage: | 0-5 mg/kg | | Administration: | Intraperitoneal or subcutaneous, single | | Result: | Followed a two-compartment model following intravenous 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 (s.c.) 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. DOI:10.1080/14787210.2018.1441024 |
|
| Company Name: |
DC Chemicals Gold
|
| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
|