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Murepavadin
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
CAS NO: 944252-63-5
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 名称
莫瑞伐定
POL7080
半岛bd体育手机客户端 介绍
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].
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.
Clinical Trial
分子量

1553.81
Formula

C73H112N22O16
CAS 号

944252-63-5
Sequence Shortening

Cyclo(AS-{d-Pro}-PTWI-{Dab}-{Orn}-{d-Dab}-{Dab}-W-{Dab}-{Dab})
中文名称

莫瑞伐定
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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