Murepavadin (POL7080)，一种 14 个氨基酸的环肽，是一种高效的特异性抗生素。Murepavadin 对P. aeruginosa表现出有效的抗菌活性。MIC50和MIC90值均为 0.12 mg/L。Murepavadin 还可以靶向脂多糖转运蛋白 D。Murepavadin 可用于细菌耐药性的研究。
| 生物活性 | Murepavadin (POL7080), a 14-amino-acid cyclic peptide, is a highly potent, specificantibiotic. Murepavadin exhibits a potent antimicrobial activity forP. aeruginosawith bothMIC50andMIC90values of 0.12 mg/L. Murepavadin also can target thelipopolysaccharide transport portin D. Murepavadin can be used for the research ofbacterialresistance[1][2]. |
| IC50& Target | MIC50: 0.12 mg/L(P. aeruginosa)[2]MIC90: 0.12 mg/L(P. aeruginosa)[2]IC50: 5.84 μM (gentamicin)[2] |
体外研究
(In Vitro) | Murepavadin has activity againstP. aeruginosawith MIC50and MIC90values both of 0.12 mg/L[2].
Murepavadin inhibits megalin-mediated uptake of gentamicin in vitro with an IC50value of 5.84 μM[2].
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体内研究
(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 ofP. aeruginosainfection[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. |
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| Clinical Trial | |
| 分子量 | |
| Formula | |
| CAS 号 | |
| Sequence Shortening | Cyclo(AS-{d-Pro}-PTWI-{Dab}-{Orn}-{d-Dab}-{Dab}-W-{Dab}-{Dab}) |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table: | | Contents | Assign value | | Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 | | Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 | | Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution: | Overall charge of peptide | Details | | Negative (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>0) | 1. Try to dissolve the peptide in water first.
2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. | | Zero (=0) | 1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
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