Murepavadin (POL7080) (TFA)，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) (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specificantibiotic. Murepavadin exhibits a potent antimicrobial activity forP. aeruginosawithMIC50andMIC90values both 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.; 0-100mg/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 | |
| 性状 | |
| Formula | |
| Sequence Shortening | Cyclo(AS-{d-Pro}-PTWI-{Dab}-{Orn}-{d-Dab}-{Dab}-W-{Dab}-{Dab}) |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 50 mg/mL(29.98 mM;Need ultrasonic) 配制储备液 | 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 |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 25 mg/mL (14.99 mM); Clear solution; Need ultrasonic and warming
*以上所有助溶剂都可在本网站选购。 |
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