Lemborexant
- Product Name
- Lemborexant
- CAS No.
- 944252-63-5
- Chemical Name
- Lemborexant
- Synonyms
- POL7080;POL-7080;POL 7080;Murepavadin acetate;Murepavadin TFA salt;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];(6S,9S,12S,15S,18S,21S,24R,27S,30S,33S,36S,39S,41aS,46aR)-18,36-Bis((1H-indol-3-yl)methyl)-12,15,21,24,30-pentakis(2-aminoethyl)-27-(3-aminopropyl)-33-((S)-sec-butyl)-39-((R)-1-hydroxyethyl)-6-(hydroxymethyl)-9-methyltriacontahydro-1H,5H-dipyrrolo[1,2-a:1',2'-d][1,4,7,10,13,16,19,22,25,28,31,34,37,40]tetradecaazacyclodotetracontine-5,8,11,14,17,20,23,26,29,32,35,38,41,46(46aH)-tetradecaone
- CBNumber
- CB63159923
- Molecular Formula
- C73H112N22O16
- Formula Weight
- 1553.84
- MOL File
- 944252-63-5.mol
Lemborexant Property
- 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
N-Bromosuccinimide Price
- Product number
- DC11273
- Product name
- Murepavadin(POL7080)
- Purity
- >98%
- Packaging
- 5mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CD22005327
- Product name
- Murepavadin
- Purity
- 97%
- Packaging
- 5mg
- Price
- $588
- Updated
- 2021/12/16
- Product number
- CD22005327
- Product name
- Murepavadin
- Purity
- 97%
- Packaging
- 10mg
- Price
- $1000
- Updated
- 2021/12/16
Lemborexant Chemical Properties,Usage,Production
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
Lemborexant Preparation Products And Raw materials
Raw materials
Preparation Products
Lemborexant Suppliers
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