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Murepavadin TFA
本产品不向个人销售,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。
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
POL7080 TFA
产品介绍
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。MIC50MIC90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].

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.
Clinical Trial
分子量

1667.83

性状

Solid

Formula

C73H112N22O16.C2HF3O2

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°C2 years
-20°C1 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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.5996 mL2.9979 mL5.9958 mL
5 mM0.1199 mL0.5996 mL1.1992 mL
10 mM0.0600 mL0.2998 mL0.5996 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。